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Cat. No. | Product Name | ||
---|---|---|---|
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; |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6152 |
PD318088
|
MEK | MAPK |
PD318088 是非 ATP 竞争性的MEK1/2变构抑制剂,是 PD184352 的结构类似物。它在MEK1 活性位点与 ATP 结合位点相邻的区域与 ATP 同时结合,可用于癌症研究。 | |||
T6785 |
BI-847325
|
Apoptosis; MEK; Aurora Kinase | Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; MAPK |
BI847325是MEK 和极光激酶 (AK)的一种选择性双重抑制剂, 对人类MEK2和AK-C 的IC50值分别为4和15 nM。 | |||
T6692 |
TAK-733
TAK733,TAK 733 |
MEK | MAPK |
TAK-733 是选择性 MEK 抑制剂,IC50为 3.2 nM。 | |||
T2708 |
SL327
SL 327,SL-327 |
MEK; DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; MAPK |
SL327 是能通过血脑屏障运输的选择性 MEK1/2 抑制剂,IC50 分别为 0.18 和 0.22 μM。 | |||
T21295 |
BIX02189
BIX 02189 |
ERK; MEK | MAPK |
BIX02189 是一种有效的选择性 MEK5 和 ERK5 抑制剂,IC50分别为 1.5 和 59 nM。 | |||
T21635 |
PD184161
|
MEK | MAPK |
PD 184161 是一种口服有效的,时间和浓度依赖的 MEK 抑制剂,IC50为10-100 nM。它诱导抑郁样行为,抑制细胞增殖并诱导细胞凋亡。 | |||
T6971 |
Ro 5126766
CH5126766,Avutometinib,VS-6766,RO5126766 |
Raf; MEK | MAPK |
Ro 5126766 (CH5126766) 是双重MEK/RAF 抑制剂,抑制BRAFV600E、CRAF、MEK 和 BRAF,IC50分别为 8.2、56、160 和 190 nM。 | |||
T2623 |
PD98059
PD 98059 |
ERK; Aryl Hydrocarbon Receptor; MEK; Autophagy | Autophagy; Immunology/Inflammation; MAPK |
PD98059 是一种 MEK 抑制剂,抑制 MEK1 和 MEK2 (IC50=2/50 μM),具有非 ATP 竞争性。PD98059 也是一种 AHR 的配体而起拮抗作用。PD98059 可以抑制细胞自噬。 | |||
T2443 |
CI-1040
PD 184352 |
Apoptosis; MEK | Apoptosis; MAPK |
CI-1040 (PD 184352) 是一种有口服活性的高度特异性MEK 小分子抑制剂,对 MEK1 的IC50值为 17 nM 。 | |||
T7610 |
GW284543
UNC10225170 |
MEK | MAPK |
GW284543 (UNC10225170) 是一个选择性的MEK5抑制剂,可降低 pERK5,并下调内源性 MYC 蛋白。 | |||
T6189 |
Mirdametinib
PD325901,PD0325901 |
Apoptosis; MEK; Autophagy | Apoptosis; Autophagy; MAPK |
Mirdametinib (PD325901) 是一种 MEK 抑制剂 (IC50=0.33 nM),具有选择性、非 ATP 竞争性和口服活性。Mirdametinib 具有抗肿瘤活性,可以抑制 p-ERK1/2 的表达并诱导细胞凋亡。 | |||
T21980 |
PD 198306
|
MEK | MAPK |
PD 198306 是一种具有抗痛觉过敏作用的 MAPK/ERK 激酶 (MEK) 选择性抑制剂。 PD 198306 可降低链脲佐菌素诱导的活性 ERK1 水平升高。 | |||
T6218 |
Selumetinib
ARRY-142886,司美替尼,AZD6244 |
Apoptosis; ERK; MEK | Apoptosis; MAPK |
Selumetinib (AZD6244) 是一种高效选择性的,非 ATP 竞争性的MEK1/2抑制剂, 抑制 MEK1 的IC50为14 nM。它抑制 MEK1/2 磷酸化水平。 | |||
T1144L |
Lidocaine Hydrochloride hydrate
|
EGFR; Sodium Channel | Angiogenesis; JAK/STAT signaling; Membrane transporter/Ion channel; Tyrosine Kinase/Adaptors |
Lidocaine Hydrochloride hydrate 是一种酰胺类局部麻醉剂,具有抗炎作用。 | |||
T5412 |
RO4987655
CH4987655,RG7167 |
MEK | MAPK |
RO4987655 (RG7167) 是一种具有口服活性和高选择性的 MEK 抑制剂,抑制MEK1/MEK2,IC50为 5.2 nM。 | |||
T6760 |
APS-2-79 hydrochloride
APS-2-79 HCl,APS-2-79 |
MEK; MAPK | MAPK |
APS-2-79 hydrochloride (APS-2-79 HCl) 是一种 KSR 依赖性的MEK 拮抗剂,可与 ATPbiotin 竞争性地结合到 KSR2-MEK1 复合物内的KSR2。它与 KSR 结合可将 KSR 处于非活性状态,使其无法再结合 RAF 和激活 MEK,从而阻断 Ras-MAPK 信号通路。 | |||
T6083 |
AZD8330
ARRY-424704,ARRY-704 |
ERK; MEK | MAPK |
AZD8330 (ARRY-704) 是非竞争性的 MEK1/MEK2抑制剂,IC50为 7 nM。 | |||
T0468 |
Lidocaine
Lignocaine,Alphacaine,Xylocaine,利多卡因 |
Apoptosis; ERK; NF-κB; MEK; Sodium Channel; Histamine Receptor | Apoptosis; GPCR/G Protein; Immunology/Inflammation; MAPK; Membrane transporter/Ion channel; Neuroscience; NF-κB |
Lidocaine (Alphacaine) 是一种酰胺衍生物,抑制涉及复杂电压和依赖性的钠通道,可用于研究室性心律失常。它通过调节 miR-145 表达和进一步抑制 MEK/ERK 和 NF-κB 信号通路来减少胃癌细胞的生长,迁移和侵袭。 | |||
T6843 |
GDC-0623
G-868,GDC0623,RG 7421,MEK inhibitor 1 |
Apoptosis; MEK | Apoptosis; MAPK |
GDC-0623 (RG 7421) 是一种 ATP 竞争性的MEK1抑制剂,Ki 值为 0.13 nM。它对 A375 细胞中 BRAFV600E 的 EC50值为 7 nM,而对 HCT116 细胞中 KRAS (G13D)的 EC50值为 42 nM。 | |||
T6223 |
U0126-EtOH
U0126 Ethanol,U0126 |
Mitophagy; Influenza Virus; MEK; Autophagy | Autophagy; MAPK; Microbiology/Virology |
U0126-EtOH (U0126 Ethanol) 是一种非 ATP 竞争性的选择性MEK1和MEK2抑制剂,IC50分别为 72 nM 和 58 nM。U0126-EtOH 可抑制自噬和线粒体自噬。 | |||
T2125 |
Trametinib
GSK1120212,曲美替尼,JTP-74057 |
Apoptosis; MEK; Autophagy | Apoptosis; Autophagy; MAPK |
Trametinib (GSK1120212) 是一种 MEK 抑制剂,抑制 MEK1 和 MEK2 (IC50=0.7/0.9 nM),具有 ATP 非竞争性和口服活性。Trametinib 可以激活自噬,诱导凋亡。 | |||
T1144 |
Lidocaine hydrochloride
Lidocaine HCL,盐酸利多卡因,Lignocaine hydrochloride,Xyloneural,Lidothesin |
Apoptosis; ERK; NF-κB; MEK; Sodium Channel | Apoptosis; MAPK; Membrane transporter/Ion channel; NF-κB |
Lidocaine hydrochloride (Lignocaine hydrochloride) 抑制涉及复杂电压和依赖性的钠通道。它通过调节 miR-145 表达和进一步抑制 MEK/ERK 和 NF-κB 信号通路来减少胃癌细胞的生长,迁移和侵袭。Lidocaine 是一种酰胺衍生物,是一种研究室性心律失常的药物和有效的肿瘤抑制剂。 | |||
T2378 |
RGB-286638 free base
|
GSK-3; MEK; JAK; CDK | Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; JAK/STAT signaling; MAPK; PI3K/Akt/mTOR signaling; Stem Cells |
RGB-286638 free base 是一种新型 CDK 抑制剂,抑制cyclin T1-CDK9、cyclin B1-CDK1、cyclin E-CDK2、cyclin D1-CDK4、cyclin E-CDK3和p35-CDK5活性,IC50分别为 1、2、3、4、5 和 5 nM。它也抑制 GSK-3β、TAK1、Jak2 和 MEK1,IC50值分别为 3、5、50和 54 nM。 | |||
T2508 |
Binimetinib
ARRY-438162,ARRY-162,MEK162 |
MEK; Autophagy | Autophagy; MAPK |
Binimetinib (ARRY-162) 是一种可口服的选择性 MEK1/2抑制剂,抑制MEK 的IC50为 12 nM。 | |||
T3623 |
Cobimetinib
可美替尼,考比替尼,RG7420,XL518,GDC-0973 |
Apoptosis; MEK | Apoptosis; MAPK |
Cobimetinib (GDC-0973) 是一种可口服的 MEK1选择性抑制剂,抑制MEK1的IC50为4.2 nM。 | |||
T6131 |
Pimasertib
AS703026,MSC1936369B,N-[(2S)-2,3-二羟基丙基]-3-[(2-氟-4-碘苯基)氨基]-4-吡啶甲酰胺,SAR 245509 |
MEK | MAPK |
Pimasertib (AS703026) 是一种高效选择性和ATP 非竞争性的MEK1/2抑制剂,可用于癌症研究。 | |||
T6636 |
Refametinib
BAY 86-97661,瑞法替尼//瑞美替尼,BAY 869766,RDEA119 |
MEK | MAPK |
Refametinib (RDEA119) 是可口服的、非 ATP 竞争和选择性的 MEK1/MEK2变构抑制剂,IC50分别为 19 和 47 nM。 | |||
T5857 |
Trametinib (DMSO solvate)
Trametinib DMSO solvate,GSK-1120212 (DMSO solvate),Trametinib dimethyl sulfoxide,JTP-74057 (DMSO solvate) |
Apoptosis; MEK | Apoptosis; MAPK |
Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate)) 是一种口服有效的 MEK 抑制剂,抑制 MEK1 和 MEK2 的 IC50分别为 2 nM。它还能激活自噬,诱导凋亡。 | |||
T9321 |
zapnometinib
ATR-002,3,4-difluoro-2-(2-chloro-4-iodophenylaMino)-benzoic acid,PD0184264,2-(2-chloro-4-iodoanilino)-3,4-difluorobenzoic acid |
Influenza Virus; MEK; Antibacterial | MAPK; Microbiology/Virology |
Zapnometinib (ATR-002) 是 CI-1040 的活性代谢物,是一种 MEK 抑制剂,IC50值为 5.7 nM,有抗流感病毒的抗病毒和抗菌活性。 | |||
T21332 |
U0126
U 0126,U-0126 |
Mitophagy; MEK; Autophagy | Autophagy; MAPK |
U0126 是一种有效的特异性非竞争性 MAP 激酶抑制剂,抑制 MEK-1 和 MEK-2,IC50 值分别为 0.07 和 0.06 μM。 U0126 抑制自噬和线粒体自噬。 | |||
T22677 |
Cobimetinib racemate
Cobimetinib (racemate),考比替尼 (外消旋体) |
MEK | MAPK |
Cobimetinib racemate (Cobimetinib (racemate)) 是 Cobimetinib 的外消旋体,是一种选择性 MEK 抑制剂。 | |||
T70317 |
BIBU-1361 dihydrochloride
|
Others | Others |
BIBU-1361 dihydrochloride is an inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase that blocks downstream EGFR signaling events such as MAPKK/MAPK activation. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
T7030 |
anemarsaponin B
知母皂苷B,知母皂苷 B |
p38 MAPK; NF-κB; MEK; COX; NO Synthase | Immunology/Inflammation; MAPK; Neuroscience; NF-κB |
Anemarsaponin B 是一种甾体皂苷,可降低iNOS 和COX-2的蛋白和 mRNA 水平,减少促炎细胞因子的表达和产生。它通过阻断 IκBα 的磷酸化来抑制NF-κB 的 p65 亚基的核转位,还抑制 MAP 激酶激酶 3/6 (MKK3/6) 和混合谱系激酶 3 的磷酸化。 | |||
T2836 |
Isorhamnetin
3-methylquercetin,3'-Methylquercetin,Isorhamnetol,异鼠李素,3'-Methoxyquercetin |
MEK; PI3K; Endogenous Metabolite | MAPK; Metabolism; PI3K/Akt/mTOR signaling |
Isorhamnetin (3-methylquercetin) 是从中草药沙棘中提取的一种类黄酮,可通过抑制MEK1和PI3K 来抑制皮肤癌。 |
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-04569 |
MEK1 Protein, Mouse, Recombinant (His & GST)
MEKK1,mitogen-activated protein kinase kinase 1,Prkmk1,M... |
Mouse | Baculovirus Insect Cells |
MEK1 Protein, Mouse, Recombinant (His & GST) is expressed in Baculovirus insect cells with His and GST tag. The predicted molecular weight is 71.3 kDa and the accession number is P31938. | |||
TMPY-04756 |
MEK1 Protein, Mouse, Recombinant
Prkmk1,MAPKK1,mitogen-activated protein kinase kina... |
Mouse | Baculovirus Insect Cells |
MEK1 Protein, Mouse, Recombinant is expressed in Baculovirus insect cells. The predicted molecular weight is 43.6 kDa and the accession number is P31938. | |||
TMPY-04364 |
MKK6 Protein, Human, Recombinant (His & GST)
MKK6,mitogen-activated protein kinase kinase 6,SAPKK3,MA... |
Human | Baculovirus Insect Cells |
MKK6 Protein, Human, Recombinant (His & GST) is expressed in Baculovirus insect cells with His and GST tag. The predicted molecular weight is 65.3 kDa and the accession number is P52564-1. | |||
TMPY-04365 |
MKK6 Protein, Human, Recombinant (S207D, T211D, His & GST)
SAPKK3,mitogen-activated protein kinase kinase 6,MKK6,MA... |
Human | Baculovirus Insect Cells |
MKK6 Protein, Human, Recombinant (S207D, T211D, His & GST) is expressed in Baculovirus insect cells with His and GST tag. The predicted molecular weight is 65.3 kDa and the accession number is P52564-1. | |||
TMPY-04749 |
MKK6 Protein, Human, Recombinant (S207D, T211D)
MAPKK6,PRKMK6,MKK6,MEK6,mitogen-activated protein k... |
Human | Baculovirus Insect Cells |
MKK6 Protein, Human, Recombinant (S207D, T211D) is expressed in Baculovirus insect cells. The predicted molecular weight is 37.7 kDa and the accession number is P52564-1. | |||
TMPY-04748 |
MKK6 Protein, Human, Recombinant
MKK6,MAPKK6,SAPKK-3,SAPKK3,PRKMK6,MEK6,mitogen-acti... |
Human | Baculovirus Insect Cells |
MKK6 Protein, Human, Recombinant is expressed in Baculovirus insect cells. The predicted molecular weight is 37.6 kDa and the accession number is A8K3Y2. | |||
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 / ... | |||
TMPY-04547 |
PBK/TOPK Protein, Human, Recombinant (His)
HEL164,Nori-3,CT84,TOPK,PDZ binding kinase,SPK |
Human | Baculovirus Insect Cells |
PDZ binding kinase (PBK), also known as TOPK (T-LAK cell-originated protein kinase), is a serine/threonine kinase related to the dual specific mitogen-activated protein kinase kinase (MAPKK) family, and has all the characteristic protein kinase subdomains and a C-terminal PDZ-binding T/SXV motif. PBK is expressed in the testis restrictedly expressed in outer cell layer of seminiferous tubules, as well as placenta. PBK may be enrolled in the activation of lymphoid cells and support testicular fun... |