584
44
7
117
10
Cat. No. | Product Name | ||
---|---|---|---|
L1610 | FDA 上市激酶抑制剂库 | 263 compounds | |
263种靶向激酶的上市药物集合,用于特定靶向激酶,可用于高通量筛选和高内涵筛选; | |||
L1400 | MAPK 抑制剂库 | 365 compounds | |
365 种与MAPK 信号通路相关的生物活性小分子化合物的特有集合,可用于高通量筛选和高内涵筛选; | |||
L1600 | 激酶抑制剂库 | 2720 compounds | |
2720 种激酶抑制剂/调节剂的独特集合,用于特定靶向激酶,可用于高通量筛选和高内涵筛选; | |||
L9410 | 共价抑制剂库 | 1920 compounds | |
1920 种小分子的独特集合,包含已发现的共价抑制剂以及包含某些共价反应基团常见弹头的分子,如氯乙酰基,2-氯丙酰基,丙烯酰基,1-丙-2-炔基,1-丁-2-炔基,酮羰基,二硫键等,可以用于共价抑制剂药物研发; | |||
L2200 | 酪氨酸激酶分子库 | 1016 compounds | |
1016 种酪氨酸激酶抑制剂的独特集合,可用于高通量筛选和高内涵筛选; | |||
L8300 | 染色质修饰分子库 | 250 compounds | |
250 种染色质化学修饰相关的生物活性小分子化合物的特有集合,用于高通量、高内涵筛选; | |||
L3700 | JAK-STAT 化合物库 | 252 compounds | |
252 个 JAK/STAT 靶点相关的小分子化合物的独特集合,用于高通量、高内涵筛选; |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T60220 |
ROS kinases-IN-1
|
ROS Kinase | Tyrosine Kinase/Adaptors |
ROS kinases-IN-1 是一种 ROS 酪氨酸激酶抑制剂,IC50 值为 1.22 μM。ROS kinases-IN-1 具有抗肿瘤活性。 | |||
T30580 |
BRD4-Kinases-IN-3
BRD4 kinases inhibitor 3,BRD4-Kinases inhibitor-3 |
Others | Others |
BRD4-Kinases-IN-3 is a dual BRD4-Kinases inhibitor that can be used as a value-added multi-targeted chemical probe for cancer therapy. | |||
T74671 |
ROS kinases-IN-2
|
ROS Kinase | Tyrosine Kinase/Adaptors |
ROS kinases-IN-2 是一种有效的 ROS kinase 抑制剂,在 10 μM 时测得抑制率为 21.53%。ROS kinases-IN-2 具有潜在的抗癌活性,可用于研究异常细胞生长。 | |||
T72504 |
Aurora Kinases-IN-3
|
Others | Others |
Aurora Kinases-IN-3 是一种具有口服活性的AURKB 抑制剂,通过破坏 AURKB 的有丝分裂定位,而不是抑制其在 Ser10 位点 H3 的磷酸化,从而诱导 AURKB 抑制活性。 | |||
T78753 |
Aurora Kinases-IN-4
|
Aurora Kinase | Cell Cycle/Checkpoint; Chromatin/Epigenetic |
Aurora Kinases-IN-4(Compound 11c)是共价ATP竞争型aurora kinaseA抑制剂,具有IC50为1.7 nM。该化合物对SJSA-1、MDA-MB-231、A549和HeLa细胞系的增殖抑制效果显著,其IC50分别为4.27、1.54、3.08和6.99 μM。Aurora Kinases-IN-4适用于三阴性乳腺癌(TNBC)的相关研究。 | |||
T62484 |
Aurora Kinases-IN-2
|
Others | Others |
Aurora Kinases-IN-2 (compound 12Aj) 是一种 Aurora 激酶的有效抑制剂 (Aurora kinases),能够作用于 Aurora A (IC50: 90 nM) 和 Aurora B (IC50: 152 nM)。Aurora Kinases-IN-2 能够调节细胞周期蛋白 B1 和 cdc2 ,将细胞周期阻滞在 G2/M 期。Aurora Kinases-IN-2 能够用于研究癌症。 | |||
T16125 |
MMV390048
|
Parasite; PI4K | Microbiology/Virology; PI3K/Akt/mTOR signaling |
MMV390048 是一种抗疟药,是一种新型化学疟原虫 PI4K 抑制剂。它与疟原虫 PI4K 的 ATP 结合位点结合,不与除人类 PIP4K2C 外的其他恶性疟原虫和人类激酶结合。 | |||
T14860 |
CaMKII-IN-1
|
CaMK; Autophagy | Autophagy; Neuroscience |
CaMKII-IN-1是高效的 CaMKII 选择性抑制剂,IC50为63nM,对 CaMKIV, MLCK, p38a, Akt1,和 PKC 这些靶点几乎无作用。 | |||
TQ0009 |
UCB9608
|
PI4K | PI3K/Akt/mTOR signaling |
UCB9608 是选择性、可口服的 PI4KIIIβ 抑制剂,IC50=11 nM,对其选择性高于 PI3KC2 α,β 和 γ。它能够增加代谢稳定性,具有良好的药代动力学特征,是一种免疫抑制剂。 | |||
T2697 |
KN-93
|
CaMK; Autophagy | Autophagy; Neuroscience |
KN-93是 Ca2+/钙调蛋白依赖性激酶 II (CaMKII) 的选择性抑制剂,Ki 为370 nM,可竞争性阻断 CaM 与激酶的结合。 | |||
T16967 |
T-00127_HEV1
|
PI4K | PI3K/Akt/mTOR signaling |
T-00127_HEV1 是有效的phosphatidylinositol 4-kinase III beta 抑制剂,IC50为 60 nM。 | |||
T12454 |
PI-273
|
Apoptosis; PI4K | Apoptosis; PI3K/Akt/mTOR signaling |
PI-273 是一种可逆的特异性磷脂酰肌醇 4-激酶抑制剂,IC50为 0.47 μM。它可抑制乳腺癌细胞的增殖,阻断细胞周期并诱导细胞凋亡。 | |||
TQ0137 |
A-484954
A 484954 |
CaMK; Parasite; Autophagy | Autophagy; Microbiology/Virology; Neuroscience |
A-484954 (A 484954) 是一种高度特异性的真核延伸因子-2 抑制剂,其 IC50值为 280 nM。 | |||
T16530 |
BF738735
|
Antiviral; PI4K | Immunology/Inflammation; PI3K/Akt/mTOR signaling |
BF738735 是有效的磷脂酰肌醇 4-激酶 IIIβ 抑制剂,IC50为 5.7 nM。 | |||
T10599 |
BRAF inhibitor
|
Raf | MAPK |
BRAF inhibitor 是B-Raf 抑制剂。 | |||
TP2310 |
Autocamtide-2-related inhibitory peptide
|
CaMK; Autophagy | Autophagy; Neuroscience |
Autocamtide-2-related inhibitory peptide 是一种高度特异性和有效的 CaMKII 抑制剂,IC50 为 40 nM。 | |||
T6605 |
NH125
|
CaMK; Virus Protease; PKA; Antibacterial; PKC; Autophagy; Antifungal | Autophagy; Chromatin/Epigenetic; Cytoskeletal Signaling; Microbiology/Virology; Neuroscience; Tyrosine Kinase/Adaptors |
NH125 是一种真核延长因子 2 激酶(eEF-2K/CaMKIII)的高效选择性抑制剂,诱导 eEF2 磷酸化,对 eEF-2K 作用的 IC50值为 60 nM。 | |||
T5421 |
KDU691
|
Parasite; PI4K | Microbiology/Virology; PI3K/Akt/mTOR signaling |
KDU691 是一种咪唑吡嗪类药物,对血阶段的裂殖体、配子体和肝期具有较强的抗寄生虫活性,它是 PI4K 抑制剂,选择性抑制双氢青蒿素预处理的恶性疟原虫。 | |||
T12468 |
PI4KIIIbeta-IN-10
|
PI3K; PI4K | PI3K/Akt/mTOR signaling |
PI4KIIIbeta-IN-10 是PI4KIIIβ抑制剂,IC50=3.6 nM。 | |||
T2616 |
PIK-93
PIK 93 |
ATM/ATR; DNA-PK; Virus Protease; PI3K; Carbonic Anhydrase; PI4K; mTOR; HSV | DNA Damage/DNA Repair; Metabolism; Microbiology/Virology; PI3K/Akt/mTOR signaling |
PIK-93 是一种合成的PI4KIIIβ抑制剂,IC50值为 19 nM,同时可抑制PI3Kγ和PI3Kα的活性,IC50值分别为 16 nM 和 39 nM。 | |||
T11224 |
Rineterkib
ERK-IN-1 |
ERK; Raf | MAPK |
Rineterkib (ERK-IN-1) 是口服有效的RAF 和ERK1/2的抑制剂,与 KRAS-突变型非小细胞肺癌、BRAF-突变型非小细胞肺癌、KRAS-突变型胰腺癌、KRAS -突变型结肠癌和 KRAS-突变型卵巢癌尤为相关。 | |||
T3546 |
STO-609
STO 609 |
CaMK; AMPK; Autophagy | Autophagy; Chromatin/Epigenetic; Neuroscience; PI3K/Akt/mTOR signaling |
STO-609 是一种特异性和细胞渗透性的 Ca2+/钙调蛋白依赖性蛋白激酶激酶抑制剂,用于重组 CaM-KKα 和 CaM-KKβ,Ki 值分别为 80 和 15 ng/mL。它抑制 Hela 细胞溶解物中的 AMP 活化蛋白激酶激酶活性,IC50值约为 0.02 g/ml。 | |||
T2694 |
KN-62
|
CaMK; P2X Receptor; Autophagy | Autophagy; Membrane transporter/Ion channel; Neuroscience |
KN-62 是一种选择性的、可逆的钙调蛋白依赖性蛋白激酶 II (CaMK-II) 抑制剂,直接与 CaMK-II 酶的钙调蛋白结合位点结合,对大鼠脑 CaMK-II 的IC50值为 0.9 μM。它是非竞争性的P2X7受体拮抗剂,IC50约为 15 nM。 | |||
T21588 |
Olomoucine
|
ERK; CDK | Cell Cycle/Checkpoint; MAPK |
Olomoucine 是 Cdk2/cyclin A、Cdc2/CyclinB、CDK2/CyclinE、CDK5/p35 和 ERK1/p44 MAP 激酶的 ATP 竞争性抑制剂,IC50 分别为 7、7、7、3 和 25 µM。 Olomoucine 调节细胞周期并表现出抗黑色素肿瘤活性。 | |||
T12469 |
PI4KIIIbeta-IN-9
|
PI3K; PI4K | PI3K/Akt/mTOR signaling |
PI4KIIIbeta-IN-9 是一种 PI4KIIIβ抑制剂,其 IC50=7 nM。它也抑制 PI3Kδ (IC50:125 nM) 和 PI3Kγ (IC50:1046 nM)。 | |||
T2295 |
SB-590885
|
Raf | MAPK |
SB590885 是一种 B-Raf 抑制剂,Ki 值为 0.16 nM,对其选择性是对 c-Raf 的 11 倍多。 | |||
T4220 |
BQR-695
BQR695,NVP-BQR695 |
PI3K; Parasite; PI4K | Microbiology/Virology; PI3K/Akt/mTOR signaling |
BQR-695 (NVP-BQR695) 是一种磷脂酰肌醇 4-激酶抑制剂,对于人类和疟原虫 PI4KIIIβ 的 IC50值分别为 80 和 3.5 nM。 | |||
T5358 |
Longdaysin
|
ERK; Casein Kinase; CDK | Cell Cycle/Checkpoint; MAPK; Metabolism; Stem Cells |
Longdaysin 是一种 CK1α 和 CK1δ 的抑制剂,IC50为5.6和8.8 µM。它还抑制ERK2,IC50值为52 µM。它是Wnt/β-catenin 信号通路的抑制剂,通过阻断CK1δ/ε依赖性 Wnt 信号通路发挥抗肿瘤作用。 | |||
T27499 |
GSK-A1
|
HCV Protease; PI4K | Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome |
GSK-A1 是 III 型磷脂酰肌醇 4-激酶 PI4KA 选择性抑制剂,pIC50为 8.5-9.8,抑制 PtdIns(4,5)P2 再合成,IC50约为 3 nM。GSK-A1有效降低 PtdIns(4)P 的水平,而对 PtdIns(4,5)P2 没影响。GSK-A1在抗丙型肝炎病毒方面有研究的潜力。 | |||
T16429 |
GNE 2861
|
PAK | Cytoskeletal Signaling |
GNE 2861 是一种 PAK 抑制剂,具有 II 组的选择性。它抑制 PAK4、PAK5 和 PAK6 的IC50值分别为7.5、36和126 nM。 | |||
T11342L |
G-5555
|
PAK | Cytoskeletal Signaling |
G-5555 是 PAK1有效抑制剂,对 PAK1 和 PAK2 的Ki 值分别为 3.7 nM 和 11 nM。 | |||
T2473 |
PLX-4720
PLX4720 |
Raf | MAPK |
PLX-4720 是一种有效且选择性的 B-Raf (V600E) 抑制剂,IC50为 13 nM,与 c-Raf-1(Y340D 和 Y341D 突变)同样有效。 | |||
T6318 |
AZ 628
|
Apoptosis; Raf | Apoptosis; MAPK |
AZ 628 是一种泛Raf 激酶抑制剂,抑制B-Raf、B-RafV600E 和c-Raf-1,IC50分别为 105、34和 29 nM。 | |||
T6840 |
FRAX486
|
PAK | Cytoskeletal Signaling |
FRAX486 是一种有效的 p21 活化激酶 (PAK) 抑制剂,对 PAK1、PAK2、PAK3 和 PAK4 的 IC50 值分别为 14、33、39 和 575 nM。 | |||
T10667 |
Calmidazolium chloride
R 24571,钙调蛋白抑制剂 |
CaMK; Autophagy | Autophagy; Neuroscience |
Calmidazolium chloride (R 24571) 是一种钙调蛋白拮抗剂,对CaM 依赖性磷酸二酯酶和钙调蛋白诱导的红细胞Ca2+转运ATP 酶活化有拮抗作用,IC50分别为0.15和0.35 μM。Calmidazolium chloride 结合CaMK 的Kd 值为3 nM。Calmidazolium chloride 在抗癌领域有研究的价值。 | |||
T3711 |
RAF709
|
Raf | MAPK |
RAF709 是RAF 抑制剂,抑制BRAF 和CRAF,IC50分别为 0.4 和 0.5 nM,具有抗肿瘤活性。 | |||
T4133 |
CCT196969
|
Raf; Src | Angiogenesis; MAPK; Tyrosine Kinase/Adaptors |
CCT196969 是泛-Raf 抑制剂,抑制B-Raf、BRafV600E 和CRAF,IC50分别为 0.1、0.04、和 0.01 μM。 | |||
TQ0048 |
BI-882370
|
Raf | MAPK |
BI-882370 是高选择性的RAF 激酶抑制剂,其结合位于 BRAF 激酶的 DFG-out 无活性构象处 (ATP 结合位点)。 它抑制 SRC 家族激酶,也抑制 BRAFV600E-mutant、WT BRAF 和 CRAF 激酶,IC50值分别为 0.4、0.8 和 0.6 nM。 | |||
T4523 |
TP-3654
|
Pim | Chromatin/Epigenetic; JAK/STAT signaling |
TP3654是一种Pim 激酶抑制剂,对Pim-1和Pim-3的Ki 值分别为5和42 nM。 | |||
T15794 |
LUT014
|
Raf | MAPK |
LUT014 是B-Raf 抑制剂,IC50值为 11.7 nM,用于减少与 EGFR 抑制剂相关限制剂量的痤疮样病变研究。 | |||
T10479 |
BAY885
|
ERK | MAPK |
BAY885 是选择性 ERK5抑制剂,IC50为 35 nM。 | |||
T5184 |
ERK5-IN-1
|
ERK | MAPK |
ERK5-IN-1 是 ERK5抑制剂,IC50为 87 nM。它也抑制 LRRK2[G2019S],IC50为 26 nM。 | |||
T6014 |
FRAX597
|
PAK | Cytoskeletal Signaling |
FRAX597 是一种有效的 ATP 竞争性 I 组 PAK 抑制剂,作用于PAK1、2和3,IC50分别为 8、13 和 19 nM。 | |||
T1953 |
L-779450
L 779450 |
Raf; Autophagy | Autophagy; MAPK |
L-779450 是一种有效的 ATP 竞争性 Raf 激酶抑制剂,IC50为 10 nM,Kd 为 2.4 nM。 | |||
T6839 |
FRAX1036
|
PAK | Cytoskeletal Signaling |
FRAX1036 是一种有效的选择性 PAK1 抑制剂,对 PAK1、PAK2 和 PAK4 的 Ki 值分别为 23.3 nM、72.4 nM 和 2.4 μM。 | |||
T5172 |
AZ304
|
c-Fms; Raf; p38 MAPK; Autophagy | Autophagy; MAPK; Tyrosine Kinase/Adaptors |
AZ304 是一种 ATP 竞争性双 BRAF 激酶抑制剂,有效抑制 BRAF (WT)、BRAF (V600E) 和野生型 CRAF,IC50值分别为79、38和68 nM。具有抗肿瘤活性。它对 p38 和 CSF1R 也有抑制作用,IC50值分别为 6 nM 和 35 nM。 | |||
T2300 |
AZD1208
|
Apoptosis; Pim; Autophagy | Apoptosis; Autophagy; Chromatin/Epigenetic; JAK/STAT signaling |
AZD1208 是一种具有口服活性的高度选择性PIM 抑制剂。 | |||
T6066 |
SCH772984
|
ERK; MEK | MAPK |
SCH772984 是高选择性和 ATP 竞争性ERK 抑制剂,对 ERK1 和 ERK2 的IC50分别为 4 和 1 nM。它在含有 BRAF 或 RAS 突变的 MAPK 抑制剂初治和 MAPK 抑制剂耐药细胞中具有抗肿瘤活性。 | |||
T15437 |
GSK3145095
|
RIP kinase | Apoptosis; NF-κB |
GSK3145095 是一种口服有效的 RIPK1 抑制剂,IC50 为 5 nM,具有潜在的免疫调节活性和抗肿瘤活性。 | |||
T3537 |
GSK583
|
RIP kinase | Apoptosis; NF-κB |
GSK583 是一种高效且特异性的 RIP2 激酶抑制剂,IC50值为 5 nM。它抑制 TNF-α 和 IL-6 的产生,IC50值为 200 nM。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TQ0201 |
Hispidulin
Dinatin |
Pim | Chromatin/Epigenetic; JAK/STAT signaling |
Hispidulin 是存在于豚草中的一种黄酮,是Pim-1抑制剂,IC50值为2.71 μM。 | |||
T6S0655 |
Corynoxeine
|
ERK | MAPK |
Corynoxeine 是从钩藤中分离的一种天然产物,是 PDGF-BB 诱导血管平滑肌细胞 (VSMCs) 增殖过程中的 ERK1/ERK2抑制剂。 | |||
TN2346 |
Mogrol
|
ERK; AMPK; STAT | Chromatin/Epigenetic; JAK/STAT signaling; MAPK; PI3K/Akt/mTOR signaling; Stem Cells |
Mogrol 是罗汉果中的一种天然产物,通过抑制 ERK1/2 和 STAT3 通路,减少 CREB 激活和激活 AMPK 信号传导发挥作用。 | |||
T8114 |
Quercetagetin
栎草亭,6-Hydroxyquercetin |
Pim | Chromatin/Epigenetic; JAK/STAT signaling |
Quercetagetin (6-Hydroxyquercetin) 是存在于万寿菊中的一种类黄酮,是一种选择性和细胞渗透性的pim-1激酶抑制,IC50为 0.34 μM,具有抗炎和抗肿瘤活性。 | |||
T3857 |
magnolin
木兰脂素,(+)-Magnolin,木兰苷 |
ERK | MAPK |
Magnolin 是辛夷的一种主要成分,靶向作用于ERK1和ERK2,IC50值分别为 87 和 16.5 nM,可抑制Ras/ERKs/RSK2信号通路。它在体内外降低肾脏氧化应激,抑制 caspase-3 活性,并增加 Bcl-2 表达,具有抗炎和抗氧化作用。 | |||
T3856 |
Tenuifoliside A
|
ERK; Others | MAPK; Others |
Tenuifoliside A 是从远志分离得到的一种天然产物,具有抗凋亡、抗抑郁、抗炎和神经保护活性。 | |||
TN3967 |
Epieriocalyxin A
|
ERK; BCL; ROS; Caspase; DNA/RNA Synthesis; JNK | Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Immunology/Inflammation; MAPK; Proteases/Proteasome |
Epieriocalyxin A 可以抑制 Caco-2 结肠癌细胞的生长。它可能是未来结肠癌治疗的潜在药物。 | |||
T3844 |
Deltonin
三角叶薯蓣皂苷 |
ERK; Others; Akt; Endogenous Metabolite | Cytoskeletal Signaling; MAPK; Metabolism; Others; PI3K/Akt/mTOR signaling |
Deltonin 是从盾叶薯蓣中得到的一种甾体皂苷,抑制ERK1/2和AKT 的活化,具有抗肿瘤活性。 | |||
T6947 |
Piperlongumine
PPLGM,荜茇酰胺,Piplartine |
Apoptosis; ERK; Ferroptosis; Reactive Oxygen Species; ROS; Antibacterial; Autophagy | Apoptosis; Autophagy; Immunology/Inflammation; MAPK; Metabolism; Microbiology/Virology; NF-κB |
Piperlongumine (Piplartine) 属于生物碱类天然产物,具有抗肿瘤、抗炎、抗氧化、抗血管生成等生物活性。Piperlongumine 可以增强 ROS 水平,诱导肿瘤细胞凋亡。 | |||
TL0016 |
Sulforaphene
油菜 |
Apoptosis; ERK; EGFR; NF-κB | Angiogenesis; Apoptosis; JAK/STAT signaling; MAPK; NF-κB; Tyrosine Kinase/Adaptors |
Sulforaphene 是从萝卜种子中分离出来的天然产物,对鹿茸幼苗的 ED50 约为 2 x 10 -4 M。它通过抑制 EGFR、p-ERK1/2、NF-κB 和其他信号促进癌细胞凋亡并抑制迁移。 | |||
TN1410 |
Asperulosidic acid
ASPA,车叶草苷酸 |
ERK; NF-κB | MAPK; NF-κB |
Asperulosidic acid (ASPA) 是从白花蛇舌草药中提取的一种环烯醚萜苷,具有抗肿瘤、抗氧化和抗炎作用。它通过抑制 NF-κB 和丝裂原活化蛋白激酶信号通路抑制炎性细胞因子释放发挥抗炎作用。 | |||
T6S0619 |
Pachymic acid
3-O-Acetyltumulosic acid,茯苓酸 |
ERK; Akt | Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling |
Pachymic acid (3-O-Acetyltumulosic acid) 是来自茯苓的一种三萜,可抑制Akt 和ERK 信号传导途径。 | |||
TMS2181 |
trans-Zeatin
(E)-Zeatin,玉米素 |
ERK; MEK; Endogenous Metabolite | MAPK; Metabolism |
trans-Zeatin ((E)-Zeatin) 是植物细胞分裂素,可抑制紫外线诱导的MEK/ERK 的活化,在细胞生长、分化和分裂中起着重要的作用。 | |||
T3876 |
Loureirin B
龙血素B,龙血素 B |
PAI-1; ERK; Potassium Channel; JNK | MAPK; Membrane transporter/Ion channel; Metabolism |
Loureirin B 是从剑叶龙血树中分离到的一种黄酮,是 PAI-1抑制剂,IC50值为 26.10 μM。它抑制 KATP,以及 ERK 和 JNK 的磷酸化,具有抗糖尿病的功效。 | |||
TN1721 |
Gypenoside L
|
ERK; p38 MAPK; Calcium Channel; NF-κB; ROS | Immunology/Inflammation; MAPK; Membrane transporter/Ion channel; Metabolism; NF-κB |
Gypenoside L 是存在于绞股蓝中的一种皂苷,可增加 SA-β-半乳糖苷酶活性,促进衰老相关分泌细胞因子的产生。它还可以激活p38和ERK MAPK 通路和NF-κB 通路以诱导衰老,具有抗肿瘤和抗炎活性。 | |||
T5727 |
CAFESTOL
咖啡醇,咖啡油醇 |
ERK; NF-κB; COX; PGE Synthase | Immunology/Inflammation; MAPK; Neuroscience; NF-κB |
Cafestol 是咖啡特有的一种二萜,可靶向 AP-1 抑制ERK,有化学预防、抗肿瘤、保肝、抗氧化和抗炎作用。它通过抑制NF-kB 活化途径强烈的抑制 PGE2的产生,还抑制 LGE 激活的 RAW264.7 细胞中的PGE2产生和环氧合酶(COX-2)的 mRNA 表达。 | |||
T2973 |
Astragaloside IV
AST-IV,黄芪甲苷IV,AS-IV,黄芪皂苷 IV |
MMP; ERK; Estrogen/progestogen Receptor; JNK | Endocrinology/Hormones; MAPK; Proteases/Proteasome |
Astragaloside IV (AS-IV) 是从黄芪中分离得到的一种皂苷,抑制ERK1/2和JNK 激活,在乳腺癌细胞 MDA-MB-231 中,下调(MMP)-2和(MMP)-9的信号通路。 | |||
T3001 |
Honokiol
和厚朴酚,NSC 293100 |
ERK; HCV Protease; MEK; Akt; Autophagy | Autophagy; Cytoskeletal Signaling; MAPK; Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome |
Honokiol (NSC-293100) 是厚朴提取物的活性成分,靶向多种信号分子,具有抗氧化,抗炎,抗血管生成和抗癌活性。它可抑制 Akt 的激活并增强 ERK1/ERK2 的磷酸化。 | |||
T5S0761 |
Nitidine chloride
|
Apoptosis; ERK; FAK; p38 MAPK; NF-κB; Topoisomerase; STAT; Parasite | Angiogenesis; Apoptosis; Cytoskeletal Signaling; DNA Damage/DNA Repair; JAK/STAT signaling; MAPK; Microbiology/Virology; NF-κB; Stem Cells; Tyrosine Kinase/Adaptors |
Nitidine chloride 是从Zanthoxylum nitidum (Roxb) DC 中分离得到的,具有抗疟疾活性。它通过多个靶点通路,起抗癌作用,抑制STAT3、DNA 拓扑异构酶1和2A、ERK 和c-Src/FAK 相关信号通路。它通过MAPK 和NF-kB 途径抑制Lps 诱导的炎性细胞因子的产生。 | |||
T7939 |
Fingolimod
2-氨基-2-[2-(4-辛基苯基)乙基]-1,3-丙二醇,FTY-720A,FTY-720,芬戈莫德 |
S1P Receptor; PAK; LPL Receptor | Cytoskeletal Signaling; GPCR/G Protein |
Fingolimod (FTY-720A) 是一种 1-磷酸鞘氨醇 (S1P) 拮抗剂,作用于 K562 和 NK 细胞,IC50为 0.033 nM。它还是pak1激活剂和免疫抑制剂。 | |||
T6S0117 |
Avicularin
Fenicularin,扁蓄苷 |
ERK | MAPK |
Avicularin (Fenicularin) 具有抗过敏、抗炎、保肝、抗氧化、抗肿瘤等活性。它能通过调节 NF-κB(p65)、COX-2 和 PPAR-γ 的活性来改善人类肝细胞癌。在 LPS 刺激的 RAW 264.7 巨噬细胞中,它通过抑制 ERK 信号通路产生抗炎活性。 | |||
T17143 |
Toyocamycin
丰加霉素,Vengicide |
Apoptosis; Others; IRE1; Antibiotic; Antifungal | Apoptosis; Cell Cycle/Checkpoint; Microbiology/Virology; Others |
Toyocamycin (Vengicide) 是放线菌类产生的腺苷类似物,为 X 盒结合蛋白 1 (XBP1) 抑制剂,抑制 IRE1α 诱导的 ATP 依赖性 XBP1 mRNA 的断裂,IC50值为 80 nM。它还诱导凋亡。 | |||
T13265 |
Urolithin B
尿石素B,3-羟基-6H-苯并[C]苯并吡喃-6-酮 |
ERK; NF-κB; Akt; Endogenous Metabolite; JNK; AMPK | Chromatin/Epigenetic; Cytoskeletal Signaling; MAPK; Metabolism; NF-κB; PI3K/Akt/mTOR signaling |
Urolithin B 是一种 ellagitannins 的肠道微生物代谢产物,具有抗炎和抗氧化作用。它也是骨骼肌质量的调节因子,通过减少 IκBα 的磷酸化和降解来抑制 NF-κB 活性,并抑制 JNK、ERK 和 Akt 的磷酸化,并增强 AMPK 的磷酸化。 | |||
TN2354 |
Methylnissolin
3-Hydroxy-9,10-dimethoxyptercarpan,黄芪紫檀烷,黄芪紫檀烷苷,3-羟基-9,10-二甲氧基紫檀烷 |
ERK; PDGFR | Angiogenesis; MAPK; Tyrosine Kinase/Adaptors |
Methylnissolin 是从黄芪中分离的一种天然产物,可抑制血小板衍生生长因子 (PDGF)-BB 诱导的细胞增殖,IC50为 10 μM。。它通过抑制ERK1/2MAP 激酶级联反应抑制 PDGF-BB 诱导的血管平滑肌细胞增殖。它还抑制 PDGF-BB 诱导的细胞外信号调节激酶 1/2 (ERIC1/2) 丝裂原活化蛋白 (MAP) 激酶的磷酸化,具有抗菌和抗癌作用。 | |||
T0646 |
5-Aminosalicylic Acid
Mesalazine,5-ASA,5-氨基水杨酸,Mesalamine |
NF-κB; Lipoxygenase; COX; Glutathione Peroxidase; Endogenous Metabolite; PAK; PPAR | Cytoskeletal Signaling; DNA Damage/DNA Repair; Immunology/Inflammation; Metabolism; Neuroscience; NF-κB |
5-Aminosalicylic Acid (5-ASA) 是一种特异性的PPARγ激动剂,还抑制 p21-激活激酶1(PAK1) 和NF-κB,具有抗炎活性。 | |||
T2532 |
Tauroursodeoxycholate
Taurolite,牛磺熊去氧胆酸,Tauroursodeoxycholic Acid,UR 906,Ursodeoxycholyltaurine,TUDCA |
Apoptosis; ERK; P450; Caspase; Endogenous Metabolite | Apoptosis; MAPK; Metabolism; Proteases/Proteasome |
Tauroursodeoxycholate (UR 906) 是一种天然的高度亲水性的三级胆汁酸。Tauroursodeoxycholate 可用于原发性胆汁性肝硬化 (PBC)、胰岛素抵抗、淀粉样变性、囊性纤维化、胆汁淤滞和肌萎缩性侧索硬化症的研究。 | |||
TCS2170 |
2,5-Dihydroxyacetophenone
Quinacetophenone,2-Acetylhydroquinone,2-5-dihydroxyacetophenone,2 ',5'-二羟基苯乙酮,Acetylhydroquinone,2,5-二羟基苯乙酮,DHAP |
ERK; NF-κB; Tyrosinase | MAPK; NF-κB; Proteases/Proteasome |
2,5-Dihydroxyacetophenone (Quinacetophenone) 是从熟地黄中分离出的一种天然产物,通过阻断 ERK1/2和 NF-κB 信号通路,抑制活化巨噬细胞中炎症介质的产生。 | |||
T4291 |
(+)-Isocorydine hydrochloride
盐酸异可利定,Isocorydine HCl |
Serine/threonin kinase; Tyrosinase | Cell Cycle/Checkpoint; Metabolism; Proteases/Proteasome |
(+)-Isocorydine hydrochloride (Isocorydine HCl) 是一种真核生物蛋白激酶抑制剂。 | |||
T22974 |
Methyl 2,5-dihydroxycinnamate
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Methyl 2,5-dihydroxycinnamate 是 erbstatin 类似物,是一种高效、稳定的 EGF 受体相关酪氨酸激酶的抑制剂。 | |||
T6169 |
Indirubin
Indigopurpurin,Indigo red,NSC 105327,Couroupitine B,靛玉红 |
Apoptosis; Raf; GSK-3; CDK | Apoptosis; Cell Cycle/Checkpoint; MAPK; PI3K/Akt/mTOR signaling; Stem Cells |
Indirubin (Couroupitine B) 是一种具有抗炎症和抗癌活性的天然产物。 | |||
T2336 |
Vitamin K2
Menatetrenone,四烯甲萘醌 |
Endogenous Metabolite | Metabolism |
Vitamin K2 (Menatetrenone) 是内源性代谢产物的一种。 | |||
T3S2390 |
Caftaric acid
trans-Caftaric acid,单咖啡酰洒石酸 |
Others | Others |
Caftaric acid (trans-Caftaric acid) 是一种具有抗氧化和抗炎作用的天然产物,具有抗致突变性,也是Src 家族激酶介导的蛋白质-蛋白质相互作用的抑制剂。 | |||
T3892 |
Isoacteoside
异麦角甾苷,Isoverbascoside |
NF-κB | NF-κB |
Isoacteoside 具有抗炎作用,通过作用于 caspase-1、丝裂原活化蛋白激酶(c-Jun N-末端激酶、p38、细胞外信号调节蛋白激酶)和核因子-kappa B 途径介导。 | |||
T0610 |
Piceatannol
白皮杉醇,trans-Piceatannol,Astringenin |
Apoptosis; Serine/threonin kinase; PKA; Syk; PKC; Autophagy | Angiogenesis; Apoptosis; Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; Metabolism; Tyrosine Kinase/Adaptors |
Piceatannol (Astringenin) 是一种Syk 抑制剂,可降低由 TNF 诱导的 iNOS 表达,可研究急性肺损伤。它是存在于各种水果和蔬菜中天然存在的多酚二苯乙烯,可诱导细胞自噬和凋亡,具有抗癌和抗炎特性。 | |||
Fr16741 |
Oxindole
2-吲哚酮,板蓝根,Indolin-2-one |
Others; HIV Protease | Microbiology/Virology; Others; Proteases/Proteasome |
Oxindole (Indolin-2-one) 是一种芳族杂环砌块,其衍生物是激酶抑制剂研究中的主要成分。 | |||
TN1440 |
Beta-Hydroxyisovalerylshikonin
|
EGFR; Tyrosine Kinases; Prostaglandin Receptor; Src; AMPK; Fatty Acid Synthase | Angiogenesis; Chromatin/Epigenetic; GPCR/G Protein; Immunology/Inflammation; JAK/STAT signaling; Metabolism; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
Beta-hydroxyisovalerylshikonin 是分离自Lithospermium radix 的天然产物,具有抑制PTK 的作用, 对 EGFR 和 v-Src 受体作用的IC50分别为 0.7 μM 和 1 μM。它对多种肿瘤细胞系均有抑制作用,可以高效诱导 NCI-H522 和 DMS114 细胞的死亡。 | |||
TN1448 |
(-)-Bornyl acetate
L-(-)-Bornyl acetate,左旋乙酸冰片酯,Bornyl acetate,(-)-乙酸龙脑酯 |
p38 MAPK; NF-κB; JNK; Antifungal | MAPK; Microbiology/Virology; NF-κB |
(-)-Bornyl acetate (L-(-)-Bornyl acetate) 是存在于牛膝草油中的一种具有抗真菌活性的 (+)-Bornyl acetate 低活性异构体。 | |||
T6S1597 |
Mulberroside A
桑皮苷 A,桑皮苷A |
TNF; Tyrosinase; Interleukin | Apoptosis; Immunology/Inflammation; Proteases/Proteasome |
Mulberroside A 是桑中的一种主要活性成分,可降低TNF-α、IL-1β和IL-6的表达,抑制 NALP3、caspase-1 和 NF-κB 的激活以及 ERK、JNK 和 p38 的磷酸化 。它抑制蘑菇酪氨酸酶,具有抗炎和抗细胞凋亡作用。 | |||
T3S0737 |
Flavokawain A
2'-羟基-4,4',6'-三甲氧基查耳酮,Flavokavain A |
Apoptosis; p38 MAPK | Apoptosis; MAPK |
Flavokawain A (Flavokavain A) 是 kava 提取物中的查耳酮,是一种抗癌试剂,具有抗肿瘤活性。它通过 Bax 蛋白依赖和线粒体依赖的凋亡途径诱导细胞凋亡,有潜力用于膀胱癌的相关研究。 | |||
T6S1684 |
8-Gingerol
|
Antioxidant; Antibacterial; TRP/TRPV Channel | Membrane transporter/Ion channel; Microbiology/Virology; oxidation-reduction |
8-Gingerol 分离自姜的根状茎,是口服有效的 TRPV1激活剂,EC50值为5.0 µM。8-Gingerol 抑制 COX-2,还能抑制体外 H. pylori 的生长。 | |||
TN3042 |
4-Hydroxycinnamamide
|
ATPase; EGFR; Potassium Channel; p38 MAPK; Calcium Channel; Sodium Channel; AMPK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; MAPK; Membrane transporter/Ion channel; Metabolism; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
4-Hydroxycinnamamide has antioxidant activity. 4-Hydroxycinnamamide derivatives are specific inhibitors of tyrosine-specific protein kinases. | |||
TN7350 |
Gynosaponin TN2
|
Others | Others |
Gynosaponin TN-2, demonstrating anti-Parkinsonian activity, mitigates L-DOPA (100 and 200 μM)-induced apoptotic cell death in pheochromocytoma 12 cells through the modulation of extracellular signal-regulated protein kinases 1 and 2 activation. | |||
T15637 |
K-252b
|
PKC | Chromatin/Epigenetic; Cytoskeletal Signaling |
K-252b is an indolocarbazole isolated from the actinomycete Nocardiopsis and is a PKC inhibitor. K-252b can be used to inhibit extracellular kinases of cells in culture because it can’t pass through the cell membrane freely. | |||
TN2775 |
2-Methoxystypandrone
|
MMP; BCL; IκB/IKK; GSK-3; TNF; NOS; NF-κB; Wnt/beta-catenin; COX; JAK; STAT | Angiogenesis; Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; Immunology/Inflammation; JAK/STAT signaling; Neuroscience; NF-κB; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells |
2-Methoxystypandrone displays an immunomodulatory effect in a cellular model, it blocks inflammatory responses by impairing NF-κB signaling to limit the inflammation and oxidative stress for preservation of BBB integrity. 2-Methoxystypandrone concomitant |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPY-04544 |
MEK2 Protein, Human, Recombinant (GST)
mitogen-activated protein kinase kinase 2,FLJ26075,MKK2,CFC4... |
Human | Baculovirus Insect Cells |
Dual specificity mitogen-activated protein kinase kinase 2, also known as MAP kinase kinase 2, MAPKK2, ERK activator kinase 2, MAPK / ERK kinase 2, MEK2 and MAP2K2, is a member of the protein kinase superfamily, STE Ser/Thr protein kinase family and MAP kinase kinase subfamily. MAP2K2 / MEK2 contains one protein kinase domain. MEK1 and MEK2 (also known as MAP2K1 and MAP2K2, respectively) are evolutionarily conserved, dual-specificity kinases that mediate Erk1 and Erk2 activation during adhesion ... | |||
TMPY-02953 |
TEM8/ANTXR1 Protein, Human, Recombinant (hFc)
ATR,TEM8,anthrax toxin receptor 1,GAPO |
Human | HEK293 Cells |
ANTXR1 contains 1 VWFA domain and belongs to the ATR family. ATR (Ataxia telangiectasia and Rad3 related) and ATM (Ataxia telangiectasia mutated) are closely related kinases that are activated by DNA damage. They are serine-threonine protein kinases and belongs to the phosphatidylinositol 3' kinase-like kinase (PIKK) family. Upon recruitment by the DNA damage binding proteins/complexes (ATRIP for ATR; MRN for ATM), ATM/ATR initiate the DNA damage checkpoint by phosphorylating a number of key pro... | |||
TMPK-00474 |
IL-22RA1 Protein, Cynomolgus, Recombinant (His)
CRF2-9,IL22R1,IL-22R-α-1,IL-22RA1,zcytoR11,IL22R,IL-22R-alph... |
Cynomolgus | HEK293 Cells |
IL-22 receptor, also known as IL-22 R alpha 1 and CRF2-9, is an approximately 65 kDa transmembrane glycoprotein in the type II cytokine receptor family (CRF).Component of the receptor for IL20, IL22 and IL24. Component of IL22 receptor formed by IL22RA1 and IL10RB enabling IL22 signaling via JAK/STAT pathways. IL22 also induces activation of MAPK1/MAPK3 and Akt kinases pathways. Component of one of the receptor for IL20 and IL24 formed by IL22RA1 and IL20RB also signaling through STATs activatio... | |||
TMPJ-00166 |
SCF Protein, Mouse, Recombinant
SCF,Hematopoietic growth factor KL,MGF,Steel factor,Mast cel... |
Mouse | E. coli |
Mouse stem cell factor (SCF), is the ligand for the receptor-type protein-tyrosine kinase KIT. It plays an essential role in the regulation of cell survival and proliferation, hematopoiesis, stem cell maintenance, gametogenesis, mast cell development, migration and function, and in melanogenesis. KITLG/SCF binding can activate several signaling pathways. It also promotes phosphorylation of PIK3R1, which is the regulatory subunit of phosphatidylinositol 3-kinase, and subsequent activation of the ... | |||
TMPY-04125 |
PTP1B Protein, Human, Recombinant (His)
protein tyrosine phosphatase, non-receptor type 1,PTP1B,PTPN... |
Human | E. coli |
PTP1B, also known as PTPN1, belongs to the protein-tyrosine phosphatase (PTP) family. PTPs catalyze the hydrolysis of the phosphate monoesters specifically on tyrosine residues. Members of the PTP family share a highly conserved catalytic motif, which is essential for the catalytic activity. PTPs are known to be signaling molecules that regulate a variety of cellular processes including cell growth, differentiation, mitotic cycle, and oncogenic transformation. PTP1B contains 1 tyrosine-protein p... | |||
TMPJ-00662 |
RANKL/TNFSF11/CD254 Protein, Human, Recombinant (E. coli)
Receptor activator of nuclear factor kappa-B ligand,Receptor... |
Human | E. coli |
CD254, also known as RANKL, TNFSF11, TRANCE, OPGL and ODF, is a type II membrane protein of the tumor necrosis factor (TNF) superfamily, and affects the immune system and control bone regeneration and remodeling. RANKL is the ligand of nuclear factor (NF)-κB (RANK). When RANKL binds to RANK, it will undergo trimerization and then bind to an adaptor molecule TNF receptor-associated factor 6 (TRAF6). This results in the activation of several downstream signaling cascades, including the NFκB, mitog... | |||
TMPJ-01210 |
IL-33 Protein, Mouse, Recombinant
Interleukin-1 family member 11,白细胞介素,NF-HEV and IL- 1F11,白介素... |
Mouse | E. coli |
Mouse Interleukin 33 (IL-33) is a 30 kDa proinflammatory cytokine which may also regulates gene transcription in producer cells. IL-33 is constitutively expressed in smooth muscle and airway epithelia. IL-33 was identified based on sequence and structural homology with IL-1 family cytokines. It is up‑regulated in arterial smooth muscle, dermal fibroblasts, and keratinocytes following IL-1 alpha or IL‑1 beta stimulation. IL-33 is structurally related to IL-1, which induces helper T cells to produ... | |||
TMPY-04572 |
MKK4 Protein, Mouse, Recombinant (His & GST)
MKK4,MEK4,PRKMK4,Sek1,JNKK1,Serk1,mitogen-activated protein ... |
Mouse | Baculovirus Insect Cells |
Dual specificity mitogen-activated protein kinase kinase 4, also known as MAP kinase kinase 4, MAPKK4, JNK-activating kinase 1, MAPK/ERK kinase 4, SAPK/ERK kinase 1, c-Jun N-terminal kinase kinase 1, JNKK, and MAP2K4, is a protein that belongs to the protein kinase superfamily, STE Ser/Thr protein kinase family and MAP kinase kinase subfamily. MAP2K4 / JNKK1 is a protein kinase that is a direct activator of MAP kinases in response to various environmental stresses or mitogenic stimuli. MAP2K4 / ... | |||
TMPJ-00412 |
VEGFR1/FLT-1 Protein, Human, Recombinant (hFc)
Vascular endothelial growth factor receptor 1,Vascular perme... |
Human | HEK293 Cells |
Human Vascular endothelial growth factor receptor 1(VEGFR-1, FLT-1) is a member of the the class III subfamily of receptor tyrosine kinases (RTKs) and Tyr protein kinase family and CSF-1/PDGF receptor subfamily. VEGFR-1 is widely expressed in human tissues including normal lung, placenta, liver, kidney, heart and brain tissues. It is specifically expressed in most of the vascular endothelial cellsand peripheral blood monocytes. VEGFR-1 contains seven Ig-like C2-type domains and one protein kinas... | |||
TMPY-04396 |
C-ABL/ABL1 Protein, Human, Recombinant (GST)
v-abl,ABL,JTK7,ABL proto-oncogene 1, non-receptor tyrosine k... |
Human | Baculovirus Insect Cells |
c-Abl belongs to the class of tyrosine kinases and is the prototype of a subfamily which includes two members, c-Abl and Arg (Abl-related gene). Both proteins are localized at the cell membrane, actin cytoskeleton and cytosol, and c-Abl is present in the nucleus as well. c-Abl is a non-receptor tyrosine kinase that participates in multiple signaling pathways linking the cell surface, cytoskeleton, and the nucleus. Recent in vitro studies have also linked c-Abl to amyloid-beta-induced toxicity an... | |||
TMPY-04378 |
MAPKAPK3 Protein, Human, Recombinant (GST)
mitogen-activated protein kinase-activated protein kinase 3,... |
Human | Baculovirus Insect Cells |
The MAPKAP kinases are a group of MAP kinase substrates that are themselves kinases. In response to activation, the MAP kinases phosphorylate downstream components on a consensus Pro-X-Ser/Thr-Pro motif. Several kinases that contain this motif have been identified and serve as substrates for the ERK and p38 MAP kinases. Mitogen-activated protein (MAP) kinase-activated protein kinase 3, also known as MAPKAPK-3 and 3pK, is a member of the Ser/Thr protein kinase family. It is widely expressed in hu... | |||
TMPK-00876 |
G-CSFR/CD114 Protein, Mouse, Recombinant (His)
CD114,G CSF R,G-CSF-R,G-CSF R,CSF3R,GCSFR,Csfgr |
Mouse | HEK293 Cells |
The Granulocyte Colony-Stimulating Factor (G-CSF) receptor, a member of the hematopoietin cytokine receptor superfamily, functions as a homodimer and requires the recruitment of cytosolic protein tyrosine kinases (PTKs) to transduce its signal. | |||
TMPY-04566 |
CAMKV Protein, Human, Recombinant (His & GST)
1G5,VACAMKL,CaM kinase-like vesicle-associated |
Human | Baculovirus Insect Cells |
CaM kinase-like vesicle-associated protein, also known as CAMKV, is a peripheral membrane protein and Cytoplasmic vesicle membrane protein which belongs to theprotein kinase superfamily and CAMK Ser/Thr protein kinase family. CAMKV contains oneprotein kinase domain. It is predominantly observed in association with the plasma membrane of soma and in neurites, both axons and dendrites. CAMKV may be associated with vesicular structures. It does not appear to have detectable kinase activity. ... | |||
TMPY-04546 |
CLK3 Protein, Human, Recombinant (GST)
PHCLK3,CDC-like kinase 3,PHCLK3/152 |
Human | Baculovirus Insect Cells |
Dual specificity protein kinase CLK3, also known as CDC-like kinase 3, and CLK3, is a member of CMGC Ser/Thr protein kinase family and Lammer subfamily. Mammalian CLK is the prototype for a family of dual specificity kinases (termed Lammer kinases) that have been conserved in evolution. CLK family members have shown to interact with, and phosphorylate, serine- and arginine-rich (SR) proteins of the spliceosomal complex, which is a part of the regulatory mechanism that enables the SR prote... | |||
TMPY-03125 |
SHP-2 Protein, Mouse, Recombinant (His)
SAP-2,Syp,PTP1D,SH-PTP2,SH-PTP3,SHP-2,PTP2C,2700084A17Rik,AW... |
Mouse | HEK293 Cells |
SHP2, also known as PTPN11, belongs to the protein-tyrosine phosphatase(PTP) family, non-receptor class 2 subfamily. PTPs catalyze the removal of phosphate groups from tyrosine residues by the hydrolysis of phosphoric acid monoesters. They dephosphorylate EGFR, JAK2 and TYK2 kinases, promoting oncogenic transformation. SHP2 is widely expressed, with highest levels in heart, brain, and skeletal muscle. SHP2 acts downstream of various receptor and cytoplasmic protein tyrosine kinases to participat... | |||
TMPY-04411 |
YES1 Protein, Human, Recombinant (His & GST)
HsT441,c-yes,YES proto-oncogene 1, Src family tyrosine kinas... |
Human | Baculovirus Insect Cells |
Proto-oncogene tyrosine-protein kinase Yes, also known as Proto-oncogene c-Yes, p61-Yes and YES1, is a cytoplasm protein that belongs to the protein kinase superfamily, Tyr protein kinase family and SRC subfamily. YES1 / c-Yes contains one protein kinase domain, one SH2 domain and one SH3 domain. It is thought that the subcellular distribution of Src-family tyrosine kinases, including c-Yes binding to the cellular membrane, is membranous and/or cytoplasmic. YES1 / c-Yes protein tyrosine kinase i... | |||
TMPY-04407 |
LOK Protein, Human, Recombinant (His)
serine/threonine kinase 10,PRO2729,LOK |
Human | E. coli |
Serine / threonine-protein kinase 1, also known as Lymphocyte-oriented kinase, STK1 and LOK, belongs to the protein kinase superfamily, STE Ser / Thr protein kinase family and STE2 subfamily. Protein kinases constitute a large superfamily of enzymes with key regulatory functions in nearly all signal transmission processes of eukaryotic cells. The Ste2 family of serine/threonine kinases plays an important role in numerous cellular functions such as growth, apoptosis, and morphogenesis. STK1 is si... | |||
TMPY-04461 |
TRIB3 Protein, Human, Recombinant (GST)
SKIP3,C20orf97,tribbles pseudokinase 3,TRB3,SINK,NIPK |
Human | Baculovirus Insect Cells |
Tribbles homolog 3, also known as Neuronal cell death-inducible putative kinase, p65-interacting inhibitor of NF-kappa-B, SINK and TRIB3, is a Nucleus protein that belongs to the protein kinase superfamily and CAMK Ser/Thr protein kinase family and Tribbles subfamily. Highest expression Of TRIB3 is in liver, pancreas, peripheral blood leukocytes and bone marrow. It is also highly expressed in a number of primary lung, colon and breast tumors. TRIB3 is expressed in spleen, thymus, and prostate an... | |||
TMPY-02264 |
LRIG1 Protein, Mouse, Recombinant (His)
LIG-1,D6Bwg0781e,leucine-rich repeats and immunoglobulin-lik... |
Mouse | HEK293 Cells |
Leucine-rich repeats and immunoglobulin-like domains 1 (LRIG1) is a tumor suppressor and a negative regulator of several receptor tyrosine kinases. Leucine-rich repeats and immunoglobulin-like domains containing protein 1 (LRIG1) is an endogenous feedback regulator of receptor tyrosine kinases (RTKs) and was recently shown to inhibit the growth of different types of malignancies. Leucine-rich repeats and immunoglobulin-like domains 1(LRIG1)is a kind of transmembrane glycoprotein, which is induce... | |||
TMPY-04558 |
NEK7 Protein, Human, Recombinant (His & GST)
NIMA-related kinase 7 |
Human | Baculovirus Insect Cells |
NIMA (never in mitosis gene a)-related kinase 7, NEK7 belongs to the NIMA subfamily, NEK Ser/Thr protein kinase family, protein kinase superfamily. NEKs (NIMA-related kinases) are mammalian serine/threonine (Ser/Thr) protein kinases structurally related to Aspergillus NIMA (Never in Mitosis, gene A), which plays essential roles in mitotic signaling. NEKs share an amino-terminal catalytic domain related to NIMA, an Aspergillus kinase involved in the control of several aspects of mitosis, and dive... | |||
TMPH-03458 |
STE11 Protein, S. cerevisiae, Recombinant
Serine/threonine-protein kinase STE11,STE11 |
Saccharomyces cerevisiae | E. coli |
Serine/threonine protein kinase required for cell-type-specific transcription and signal transduction in yeast. It is thought that it phosphorylates the STE7 protein kinase which itself, phosphorylates the FUS3 and or KSS1 kinases. STE11 Protein, S. cerevisiae, Recombinant is expressed in E. coli expression system. The predicted molecular weight is 33.5 kDa and the accession number is P23561. | |||
TMPH-02272 |
JAK1 Protein, Human, Recombinant (E. coli, His)
Tyrosine-protein kinase JAK1,JAK1,Janus kinase 1 |
Human | E. coli |
Tyrosine kinase of the non-receptor type, involved in the IFN-alpha/beta/gamma signal pathway. Kinase partner for the interleukin (IL)-2 receptor as well as interleukin (IL)-10 receptor. Directly phosphorylates STAT but also activates STAT signaling through the transactivation of other JAK kinases associated with signaling receptors. | |||
TMPH-02278 |
PTPN5 Protein, Human, Recombinant (His & SUMO)
PTPN5,Neural-specific protein-tyrosine phosphatase,Tyrosine-... |
Human | E. coli |
May regulate the activity of several effector molecules involved in synaptic plasticity and neuronal cell survival, including MAPKs, Src family kinases and NMDA receptors. PTPN5 Protein, Human, Recombinant (His & SUMO) is expressed in E. coli expression system with N-6xHis-SUMO tag. The predicted molecular weight is 45.5 kDa and the accession number is P54829. | |||
TMPY-04460 |
OXSR1 Protein, Human, Recombinant (GST)
OSR1,oxidative stress responsive 1 |
Human | Baculovirus Insect Cells |
Oxidative stress-responsive 1 protein (OXSR1), also known as Serine/threonine-protein kinase OSR1, is a member of the Ser/Thr protein kinase family of proteins. OXSR1 regulates downstream kinases in response to environmental stress, and may play a role in regulating the actin cytoskeleton. OXSR1 is a 58 kDa protein of 527 amino acids that is widely expressed in mammalian tissues and cell lines. The amino acid (aa) sequence of the predicted OXSR1 protein is 39% identical to that of human SOK1. Of... | |||
TMPY-04397 |
PAK-3 Protein, Human, Recombinant (His)
PAK3β,hPAK3,bPAK,PAK3beta,MRX30,MRX47,CDKN1A,p21 protein (Cd... |
Human | Baculovirus Insect Cells |
PAK3 is a member of PAK proteins, a family of serine/threonine p21-activating kinases, serve as effectors of small Rho GTPases Cdc42 and RAC and have been implicated in a wide range of biological activities. There are six mammalian PAKs which can be divided into two groups: group I PAKs (PAK1-3) and group II PAKs (PAK4-6). Although the two PAK groups are architecturally similar there are differences in their mode of regulation suggesting their cellular functions are likely to be different. Group... | |||
TMPY-05095 |
RAF1 Protein, Human, Recombinant (His & GST)
Raf-1 proto-oncogene, serine/threonine kinase,CRAF,NS5,CMD1N... |
Human | Baculovirus Insect Cells |
RAF1 gene is the cellular homolog of viral raf gene (v-raf). The encoded protein is a MAP kinase kinase kinase (MAP3K), which functions downstream of the Ras family of membrane associated GTPases to which it binds directly. Once activated, the cellular RAF1 protein can phosphorylate to activate the dual specificity protein kinases MEK1 and MEK2, which in turn phosphorylate to activate the serine/threonine specific protein kinases, ERK1 and ERK2. Activated ERKs are pleiotropic effectors of cell p... | |||
TMPY-04260 |
p38 Protein, Human, Recombinant (His)
mitogen-activated protein kinase 14,CSPB1,PRKM14,RK,p38α,CSB... |
Human | Baculovirus Insect Cells |
MAPK14 contains 1 protein kinase domain and belongs to the MAP kinase family. MAP kinases act as an integration point for multiple biochemical signals and are involved in a wide variety of cellular processes such as proliferation, differentiation, transcription regulation, and development. MAPK14 can be detected in the brain, heart, placenta, pancreas, and skeletal muscle and it is expressed to a lesser extent in the lung, liver, and kidney. MAPK14 is activated by various environmental stresses ... | |||
TMPY-04402 |
CSNK1G1 Protein, Human, Recombinant (His & GST)
CK1γ1,casein kinase 1, gamma 1,casein kinase 1, γ1,CK1gamma1 |
Human | Baculovirus Insect Cells |
Casein kinase I isoform gamma-1, also known as CSNK1G1, is a member of the protein kinase superfamily, CK1 Ser/Thr protein kinase family and casein kinase I subfamily. Thecasein kinase I family of protein kinases are serine / threonine-selective enzymes that function as regulators ofsignal transductionpathways in most eukaryotic cell types. Casein has been used as a substrate since the earliest days of research on protein phosphorylation. Casein kinase activity associated with the endopla... | |||
TMPY-03442 |
MOB4A/MOB1B Protein, Human, Recombinant (GST)
MOB kinase activator 1B,MOBKL1A,MATS2,MOB4A |
Human | E. coli |
MST1 and MST2 are the mammalian Ste2-related protein kinases most closely related to Drosophila Hippo, a major regulator of cell proliferation and survival during development. Overexpression of MST1 or MST2 in mammalian cells is proapoptotic. MST1 and MST2 activity increase during mitosis, especially in nocodazole-arrested mitotic cells, where these kinases exhibit an increase in both abundance and activation. MST1 and MST2 also can be activated nonphysiologically by okadaic acid or H2O2. The MO... | |||
TMPH-02273 |
JAK1 Protein, Human, Recombinant (His)
JAK1,Janus kinase 1,Tyrosine-protein kinase JAK1 |
Human | P. pastoris (Yeast) |
Tyrosine kinase of the non-receptor type, involved in the IFN-alpha/beta/gamma signal pathway. Kinase partner for the interleukin (IL)-2 receptor as well as interleukin (IL)-10 receptor. Directly phosphorylates STAT but also activates STAT signaling through the transactivation of other JAK kinases associated with signaling receptors. | |||
TMPH-02209 |
TRAF5 Protein, Human, Recombinant (His & SUMO)
TRAF5,RING finger protein 84,TNF receptor-associated factor ... |
Human | E. coli |
Adapter protein and signal transducer that links members of the tumor necrosis factor receptor family to different signaling pathways by association with the receptor cytoplasmic domain and kinases. Mediates activation of NF-kappa-B and probably JNK. Seems to be involved in apoptosis. Plays a role in mediating activation of NF-kappa-B by EIF2AK2/PKR. | |||
TMPH-01581 |
KRT1 Protein, Human, Recombinant (His)
Keratin, type II cytoskeletal 1,67 kDa cytokeratin,Keratin-1... |
Human | E. coli |
May regulate the activity of kinases such as PKC and SRC via binding to integrin beta-1 (ITB1) and the receptor of activated protein C kinase 1 (RACK1). In complex with C1QBP is a high affinity receptor for kininogen-1/HMWK. KRT1 Protein, Human, Recombinant (His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weight is 69.9 kDa and the accession number is P04264. | |||
TMPH-02758 |
LIMS1 Protein, Mouse, Recombinant (His)
LIM and senescent cell antigen-like-containing domain protei... |
Mouse | Baculovirus Insect Cells |
Adapter protein in a cytoplasmic complex linking beta-integrins to the actin cytoskeleton, bridges the complex to cell surface receptor tyrosine kinases and growth factor receptors. Involved in the regulation of cell survival, cell proliferation and cell differentiation. LIMS1 Protein, Mouse, Recombinant (His) is expressed in Baculovirus insect cells with N-10xHis tag. The predicted molecular weight is 39.6 kDa and the accession number is Q99JW4. | |||
TMPH-02905 |
TRPC1 Protein, Mouse, Recombinant (His)
Transient receptor protein 1,Short transient receptor potent... |
Mouse | E. coli |
Thought to form a receptor-activated non-selective calcium permeant cation channel. Probably is operated by a phosphatidylinositol second messenger system activated by receptor tyrosine kinases or G-protein coupled receptors. Seems to be also activated by intracellular calcium store depletion. TRPC1 Protein, Mouse, Recombinant (His) is expressed in E. coli expression system with N-10xHis tag. The predicted molecular weight is 94.0 kDa and the accession number is Q61056. | |||
TMPJ-00534 |
hFcgR4 Protein, Mouse, Recombinant (His)
Low Affinity Immunoglobulin γ Fc Region Receptor IV,FcgR4,Lo... |
Mouse | HEK293 Cells |
Fcgr4, also known as CD16-2, is one of the receptors for Fc region of IgG which involve in immune responses. Fcgr4 mainly functions in cellular response to lipopolysaccharide, NK T cell proliferation, regulation of sensory perception of pain, wound healing etc. Three groups are included for Fc γ receptors (FcR), and they are Fc γ RI (CD64), Fc γ RII (CD32), and Fc γ RIII (CD16). Among these, CD64 possess high affinity even for monomeric IgG, while CD32 and CD16 display a relative lower affinity ... | |||
TMPH-02277 |
PTPN11 Protein, Human, Recombinant (T253M & Q257L, His)
Protein-tyrosine phosphatase 1D,Tyrosine-protein phosphatase... |
Human | E. coli |
Acts downstream of various receptor and cytoplasmic protein tyrosine kinases to participate in the signal transduction from the cell surface to the nucleus. Positively regulates MAPK signal transduction pathway. Dephosphorylates GAB1, ARHGAP35 and EGFR. Dephosphorylates ROCK2 at 'Tyr-722' resulting in stimulation of its RhoA binding activity. Dephosphorylates CDC73. Dephosphorylates SOX9 on tyrosine residues, leading to inactivate SOX9 and promote ossification. | |||
TMPJ-00406 |
EphA8 Protein, Human, Recombinant (His)
EPH- and ELK-related tyrosine kinase,EPH receptor A8,HEK3,Ep... |
Human | HEK293 Cells |
EphA8, also known as Hek3 and Eek, is a 120 kDa glycosylated member of the Eph family of transmembrane receptor tyrosine kinases. The A and B classes of Eph proteins are distinguished by Ephrin ligand binding preference but have a common structural organization. Eph-Ephrin interactions are widely involved in the regulation of cell migration, tissue morphogenesis, and cancer progression. Receptor tyrosine kinase which binds promiscuously GPI-anchored ephrin-A family ligands residing on adjacent c... | |||
TMPJ-01335 |
MOB1A Protein, Human, Recombinant (His)
C2orf6,MOB4B,Mob1A,MOBK1B,Mps One Binder Kinase Activator-li... |
Human | E. coli |
MOB Kinase Activator 1A (MOB1A) belongs to the MOB1/phocein family, which acts as an activator of LATS1/2 in the Hippo signaling pathway, plays a key role in organ size control and tumor suppression by restricting proliferation and promoting apoptosis. MOBKL1B stimulates the kinase activity of STK38 and STK38L. MOBKL1B binds to and regulate downstream targets such as the NDR-family protein kinases and LATS1 kinase. | |||
TMPJ-00224 |
EFNB2 Protein, Mouse, Recombinant (hFc & His)
Ephrin-B2,Htkl,Lerk5.,ELF-2,Epl5,Eplg5,EPH-related receptor ... |
Mouse | HEK293 Cells |
Ephrin-B2 is a single-pass type I membrane protein and it contains 1 ephrin RBD (ephrin receptor-binding) domain. Ephrin-B2 belongs to the ephrin (EPH) family and it is cell surface transmembrane ligand for Eph receptors, a family of receptor tyrosine kinases which are crucial for migration, repulsion and adhesion during neuronal, vascular and epithelial development. The ephrins and EPH-related receptors contain the largest subfamily of receptor protein-tyrosine kinases and have been associated ... | |||
TMPJ-00315 |
ACVR2A Protein, Human, Recombinant (hFc & His)
ACTR-IIA,Activin Receptor Type IIA,ACTRIIA,Activin Receptor ... |
Human | HEK293 Cells |
Activin Receptor Type-2A is a protein that in humans is encoded by the ACVR2A gene. ACVR2A is an activin type 2 receptor. This gene encodes activin A type II receptor. Activins are dimeric growth and differentiation factors which belong to the transforming growth factor-beta (TGF-beta) superfamily of structurally related signaling proteins. Activins signal through a heteromeric complex of receptor serine kinases which include at least two type I (I and IB) and two type II (II and IIB) receptors.... | |||
TMPY-04443 |
NEK3 Protein, Mouse, Recombinant (His & GST)
NIMA-related kinase 3 |
Mouse | Baculovirus Insect Cells |
NEK3 (NIMA (never in mitosis gene a)-related expressed kinase 3), contains 1 protein kinase domain and is a member of the NimA (never in mitosis A) family of serine/threonine protein kinases. Members of the NEK family of protein kinases share high amino acid homology with NIMA (never in mitosis gene a). NEK3 differs from other NimA family members in that it is not the cell cycle-regulated and is found primarily in the cytoplasm. It is activated by prolactin stimulation, leading to phosphorylatio... | |||
TMPH-02961 |
JAK1 Protein, Mouse, Recombinant (His)
Janus kinase 1,Jak1,Tyrosine-protein kinase JAK1 |
Mouse | E. coli |
Tyrosine kinase of the non-receptor type, involved in the IFN-alpha/beta/gamma signal pathway. Kinase partner for the interleukin (IL)-2 receptor as well as interleukin (IL)-10 receptor. Directly phosphorylates STAT but also activates STAT signaling through the transactivation of other JAK kinases associated with signaling receptors. JAK1 Protein, Mouse, Recombinant (His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weight is 39.1 kDa and the accession numb... | |||
TMPH-01265 |
PELI3 Protein, Human, Recombinant (His)
PELI3,E3 ubiquitin-protein ligase pellino homolog 3 |
Human | E. coli |
E3 ubiquitin ligase catalyzing the covalent attachment of ubiquitin moieties onto substrate proteins. Involved in the TLR and IL-1 signaling pathways via interaction with the complex containing IRAK kinases and TRAF6. Mediates 'Lys-63'-linked polyubiquitination of IRAK1. Can activate AP1/JUN and ELK1. Not required for NF-kappa-B activation. PELI3 Protein, Human, Recombinant (His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weight is 54.8 kDa and the access... | |||
TMPY-04554 |
JNK1 Protein, Human, Recombinant (GST)
PRKM8,JNK,JNK-46,JNK21B1/2,JNK1A2,mitogen-activated protein ... |
Human | Baculovirus Insect Cells |
Mitogen-activated protein kinase 8 (MAPK8), also known as JNK1, is a member of the MAP kinase family. MAP kinases act as an integration point for multiple biochemical signals and are involved in a wide variety of cellular processes such as proliferation, differentiation, transcription regulation, and development. The protein kinases JNK1 has been found to serve as critical molecular links between obesity, metabolic inflammation, and disorders of glucose homeostasis. It is critically involved in ... | |||
TMPY-04423 |
CAMKI gamma/CAMK1G Protein, Human, Recombinant (His & GST)
VWS1,RP1-272L16.2,calcium/calmodulin-dependent protein kinas... |
Human | Baculovirus Insect Cells |
Calmodulin-Dependent Protein Kinase (CaM Kinase) is a kind of protein phosphorylate multiple downstream targets. Concentration of cytosolic calcium functions as a second messenger that mediates a wide range of cellular responses. Calcium binds to calcium binding proteins (calmodulin/CaM) and stimulates the activity of a variety of enzymes, including CaM kinases referred to as CaM-kinases (CaMKs), such as CaMKI, CaMKII, CaMKIV and CaMKK. Calmodulin-dependent protein kinase CL3/CaMKIγ is a membera... | |||
TMPK-00578 |
ROR2 Protein, Human, Recombinant (aa 34-403, His & Avi), Biotinylated
BDB1,NTRKR2,ROR2,BDB |
Human | HEK293 Cells |
ROR2 (Receptor Tyrosine Kinase-like Orphan Receptor 2) is a member of the ROR family of receptor tyrosine kinases and is important for skeletal development, including bone and cartilage formation, as well as for the development of the central nervous system. Mature human ROR2 contains a 369 amino acid (aa) extracellular domain (ECD) and a 518 aa cytoplasmic tail containing an tyrosine kinase domain. ROR2 Protein, Human, Recombinant (aa 34-403, His & Avi), Biotinylated is expressed in HEK293 mamm... | |||
TMPK-00566 |
ROR2 Protein, Cynomolgus, Recombinant (His)
BDB,BDB1,NTRKR2,ROR2 |
Cynomolgus | HEK293 Cells |
ROR2 (Receptor Tyrosine Kinase-like Orphan Receptor 2) is a member of the ROR family of receptor tyrosine kinases and is important for skeletal development, including bone and cartilage formation, as well as for the development of the central nervous system. Mature human ROR2 contains a 369 amino acid (aa) extracellular domain (ECD) and a 518 aa cytoplasmic tail containing an tyrosine kinase domain. ROR2 Protein, Cynomolgus, Recombinant (His) is expressed in HEK293 mammalian cells with C-His tag... | |||
TMPY-04542 |
CDK2 Protein, Human, Recombinant (His)
CDKN2,cyclin-dependent kinase 2,p33(CDK2) |
Human | Baculovirus Insect Cells |
CDK2 is a member of the Ser/Thr protein kinase family. This protein kinase is highly similar to the gene products of S. cerevisiae cdc28, and S. pombe cdc2. It is a catalytic subunit of the cyclin-dependent protein kinase complex, whose activity is restricted to the G1-S phase, and essential for cell cycle G1/S phase transition. Cdks (cyclin-dependent kinases) are heteromeric serine/threonine kinases that control progression through the cell cycle in concert with their regulatory subunits, the c... | |||
TMPH-01699 |
SMAD2 Protein, Human, Recombinant (His & SUMO)
JV18-1,SMAD2,SMAD family member 2,Mothers against decapentap... |
Human | E. coli |
Receptor-regulated SMAD (R-SMAD) that is an intracellular signal transducer and transcriptional modulator activated by TGF-beta (transforming growth factor) and activin type 1 receptor kinases. Binds the TRE element in the promoter region of many genes that are regulated by TGF-beta and, on formation of the SMAD2/SMAD4 complex, activates transcription. May act as a tumor suppressor in colorectal carcinoma. Positively regulates PDPK1 kinase activity by stimulating its dissociation from the 14-3-3... | |||
TMPK-00579 |
ROR2 Protein, Human, Recombinant (hFc)
BDB,NTRKR2,BDB1,ROR2 |
Human | HEK293 Cells |
ROR2 (Receptor Tyrosine Kinase-like Orphan Receptor 2) is a member of the ROR family of receptor tyrosine kinases and is important for skeletal development, including bone and cartilage formation, as well as for the development of the central nervous system. Mature human ROR2 contains a 369 amino acid (aa) extracellular domain (ECD) and a 518 aa cytoplasmic tail containing an tyrosine kinase domain. ROR2 Protein, Human, Recombinant (hFc) is expressed in HEK293 mammalian cells with C-hFc tag. The... | |||
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Cat. No. | Product Name | Target | Signaling Pathways |
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T11640 |
Imatinib-d8
CGP-57148B D8,STI571 D8 |
Others | Others |
Imatinib D8 is a deuterium-labeled Imatinib. Imatinib is an orally bioavailable tyrosine kinases inhibitor that inhibits BCR/ABL, PDGFR, v-Abl, and c-kit kinase activity. | |||
T11639 |
Imatinib D4
CGP-57148B D4,STI571 D4 |
Others | Others |
Imatinib D4 is a deuterium-labeled Imatinib. Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, PDGFR, v-Abl, and c-kit kinase activity. | |||
TMID-0288 |
Apatinib-d8
|
||
Apatinib-d8 是 Apatinib 的氘代化合物。Apatinib 的 CAS 号为 811803-05-1。Apatinib 是一种口服生物可利用的特异性 VEGFR2 抑制剂 (IC50: 1 nM)。此外,该试剂温和地抑制 c-Kit 和 c-SRC 酪氨酸激酶。 | |||
T37044 |
1,2-Dioleoyl-rac-glycerol-13C3
1,2-Dioleoyl-rac-glycerol-13C3 |
||
1,2-Dioleoyl-rac-glycerol-13C3 is intended for use as an internal standard for the quantification of 1,2-dioleoyl-rac-glycerol by GC- or LC-MS. 1,2-dioleoyl-rac-glycerol is a diacylglycerol that contains oleic acid at the sn-1 and sn-2 positions. It effectively binds the C1 domain to activate conventional protein kinase C forms and serves as a substrate for diacylglycerol kinases and multisubstrate lipid kinase.1,2,3 |1. Yamaguchi, Y., Shirai, Y., Matsubara, T., et al. Phosphorylation and up-reg... | |||
TMIJ-0261 |
Baricitinib-d5
|
||
Baricitinib-d5 是 Baricitinib 的氘代化合物。Baricitinib 的 CAS 号为 1187594-09-7。Baricitinib 是一种选择性,可口服的JAK1和JAK2抑制剂,IC50分别为5.9 nM 和 5.7 nM,具有潜在的抗炎、免疫调节和抗肿瘤活性。 | |||
T70394 |
Deucravacitinib HCl
|
||
Deucravacitinib HCl is a Highly Potent and Selective Allosteric Inhibitor of TYK2. BMS-986165 Blocks Il-12, IL-23 and type I Interferon Signaling and Provides for Robust Efficacy in Preclinical Models of Inflammatory Bowel Disease. MS-986165 potently binds to the Tyk2 pseudokinase domain (Ki = 0.02 nM), and is highly selective against a panel of 265 kinases and pseudokinases. The compound potently inhibited IL-23-, IL-12-, and Type I interferon-driven cellular signaling and transcriptional resp... | |||
TMIJ-0333 |
Nintedanib-d8
|
||
Nintedanib-d8 是 Nintedanib 的氘代化合物。Nintedanib 的 CAS 号为 656247-17-5。Nintedanib 是一种有效的三重血管激酶抑制剂,能够抑制VEGFR1 (IC50:34 nM)、VEGFR2 (IC50:13 nM)、VEGFR3 (IC50:13 nM),FGFR1 (IC50:69 nM)、FGFR2 (IC50:37 nM)、FGFR3 (IC50:108 nM),PDGFRα (IC50:59 nM)、PDGFRβ (IC50:65 nM)。 | |||
TMIH-0393 |
Nintedanib-13C-d3
|
||
Nintedanib-13C-d3 是 Nintedanib 的 13C 和氘代化合物。Nintedanib 的 CAS 号为 656247-17-5。Nintedanib 是一种有效的三重血管激酶抑制剂,能够抑制VEGFR1 (IC50:34 nM)、VEGFR2 (IC50:13 nM)、VEGFR3 (IC50:13 nM),FGFR1 (IC50:69 nM)、FGFR2 (IC50:37 nM)、FGFR3 (IC50:108 nM),PDGFRα (IC50:59 nM)、PDGFRβ (IC50:65 nM)。 | |||
TMIJ-0115 |
Crizotinib-d5
|
||
Crizotinib-d5 是 Crizotinib 的氘代化合物。Crizotinib 的 CAS 号为 877399-52-5。Crizotinib 是 c-MET 和 ALK 受体的 ATP 竞争性小分子酪氨酸激酶抑制剂,IC50为 8和20 nM。在细胞的实验中,它抑制 NPM-ALK 的酪氨酸磷酸化和 c-Met 的酪氨酸磷酸化。它也是ROS1抑制剂。它有肿瘤生长抑制作用。 | |||
TMIH-0065 |
Acalabrutinib-d4
|
||
Acalabrutinib-d4 是 Acalabrutinib 的氘代化合物。Acalabrutinib 的 CAS 号为 1420477-60-6。Acalabrutinib 是一种不可逆的、高效的、具有口服活性、选择性的第二代BTK抑制剂。它与 BTK 的 ATP 结合口袋中的 Cys481 共价结合。它在慢性淋巴细胞性白血病 (CLL) 小鼠模型中显示出强大的靶向作用和功效。 |