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Targets Recommended: STAT

896

抑制剂 & 化合物

22

天然产物

7

化合物库

3

重组蛋白

6

同位素标记化合物

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Cat. No. Product Name
L9411 半胱氨酸共价化合物库

70 compounds
半胱氨酸共价库包含 70 个化合物。
LF8700 共价片段化合物库LF

6500 compounds
The resulting Library comprises over 4,000 small-molecule compounds for covalent fragment screening efforts.
L2152 靶向治疗药物库

119 compounds
119 个肿瘤靶向治疗药物,可以用于高通量和高内涵筛选;
L9610 环肽库

80 compounds
80 种环肽分子,可用于高通量和高内涵筛选;
L7400 钠通道分子库

118 compounds
118 种钠通道相关化合物的独特集合,可用于高通量筛选和高内涵筛选;
L9600 多肽分子库

791 compounds
791 种多肽类分子,可用于多肽药物开发及信号转导通路和作用机制研究;
DO2200 共价抑制剂库CD

12000 compounds
数量多:超过12000种共价结合化合物,并且数量在持续增加;

化合物库

半胱氨酸共价化合物库
Cat.No: L9411
Compounds: 70
共价片段化合物库LF
Cat.No: LF8700
Compounds: 6500
靶向治疗药物库
Cat.No: L2152
Compounds: 119
环肽库
Cat.No: L9610
Compounds: 80
钠通道分子库
Cat.No: L7400
Compounds: 118
多肽分子库
Cat.No: L9600
Compounds: 791
共价抑制剂库CD
Cat.No: DO2200
Compounds: 12000
Cat. No. Product Name Target Signaling Pathways
T9339 Stafia-1

STAT JAK/STAT signaling; Stem Cells
Stafia-1 是STAT5a 抑制剂,Ki 为 10.9 μM,IC50 为 22.2 μM。它与 STAT5b 和其他 STAT 家族成员相比,显示出高选择性。
T11960 MBM-55

GSK-3; MAPK; DYRK; Akt; Chk; Bcr-Abl; CDK; S6 Kinase; Aurora Kinase Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors
MBM-55 是一种有效的中心体相关激酶 2 (NEK2) 抑制剂,IC50 为 1 nM。 MBM-55 通过诱导细胞周期停滞和凋亡有效抑制癌细胞的增殖。
T9470 HPK1-IN-7

MAPK MAPK
HPK1-IN-7 是一种口服有活性的、有效的HPK1(造血祖细胞激酶1, MAP4K1) 抑制剂,其IC50值为2.6 nM,具有强大的家族及激酶组选择性。它对 IRAK4 (59 nM) 和 GLK (140 nM) 具有选择性。当它与抗 PD1联合使用时,对 MC38 同基因肿瘤模型表现出极大的疗效。
T4199 Desmethyl-VS-5584

PI3K; mTOR PI3K/Akt/mTOR signaling
Desmethyl-VS-5584 是 VS-5584 的二甲基类似物。其中VS-5584 是mTOR/PI3K 抑制剂,专门针对于吡啶 [2,3-d] 嘧啶结构。
T28352 PDE9-IN-(S)-C33

(S)-C33

PDE Metabolism
PDE9-IN-(S)-C33 ((S)-C33) 是一种有效的选择性 PDE9 抑制剂 (IC50 = 11 nM)。 PDE9-IN-(S)-C33 可用于中枢神经系统疾病和糖尿病的相关研究。
T9020 GSK620

Epigenetic Reader Domain Chromatin/Epigenetic
GSK620 是一种有口服活性的泛BD2抑制剂,在人全血中表现出抗炎表型,有良好的广谱选择性、可开发性和体内口服药代动力学。它对 BET-BD2 家族蛋白具有高度选择性,其选择性超过所有其他 BET 溴结构域 200 倍以上。
T11696 Ivachtin

Caspase-3 Inhibitor VII

Caspase Apoptosis; Proteases/Proteasome
Ivachtin (Caspase-3 Inhibitor VII) 是一种非肽,非竞争性和可逆的caspase-3抑制剂,IC50为 23 nM。它是其余胱天蛋白酶的适度抑制剂。
T28628 RVX-297

RVX297

Epigenetic Reader Domain Chromatin/Epigenetic
RVX-297 是口服具有活性的,对BD2有选择性的BET 高效抑制剂,作用于BRD2(BD2)、BRD3(BD2)、BRD4(BD2) 的IC50分别为 0.08、0.05、0.02 μM。它能够阻碍多种免疫细胞炎症基因的表达,对临床前模型急性炎症及自身免疫均有效。
T21331 SAR-020106

Chk Cell Cycle/Checkpoint
SAR-020106 是一种强效、ATP 竞争性和选择性 CHK1 抑制剂,IC50为 13.3 nM。它对 CHK2 具有良好的选择性,可通过选择抗癌药物增强抗肿瘤活性。
T5405 BI-1347

CDK Cell Cycle/Checkpoint
BI-1347 是一种有效的、选择性的 CDK8/cyclinC 抑制剂,IC50值为 1 nM,可抑制肿瘤生存。
T9564 IRE1α kinase-IN-1

IRE1 Cell Cycle/Checkpoint
IRE1α kinase-IN-1 是IRE1α 的选择性抑制剂(IC50为 77 nM),对 IRE1α 的选择性高于 IRE1β 亚型 100 倍。它抑制内质网诱导的 IRE1α 寡聚和自磷酸化,并抑制 IRE1α RNase 活性 (IC50=80 nM)。
T1885 Siramesine hydrochloride

Lu 28-179 hydrochloride,西拉美新盐酸盐

Ferroptosis; Sigma receptor; lysosomal autophagy Apoptosis; Autophagy; GPCR/G Protein
Siramesine hydrochloride (Lu 28-179 hydrochloride) 是一种选择性 sigma-2 受体激动剂,可引发 Y 细胞的细胞死亡并在体内表现出有效的抗癌活性。Siramesine 对 sigma-2 受体具有亚纳摩尔亲和力,并且对 sigma-2 受体的选择性是 sigma-1 受体的 140 倍。
T6658 SB-408124

N-(6,8-二氟-2-甲基-4-喹啉)- N-[4-(二甲氨基)苯基]尿素

OX Receptor GPCR/G Protein; Neuroscience
SB408124 是一种 OX1 受体的非肽拮抗剂,在全细胞和膜中的 Ki 值分别为 57 和 27 nM,其选择性是 OX2 受体的 50 倍。
T15418 GS-6201

CVT-6883

Adenosine Receptor GPCR/G Protein; Neuroscience
GS-6201 (CVT-6883) 是选择性腺苷 A2B 受体拮抗剂。它对人腺苷 A2B 受体具有高亲和力和选择性 (Ki=22 nM)。它降低了小鼠急性心肌梗死后心脏中 caspase-1 的活性,并减弱了心脏重塑。它减弱了致敏小鼠 NECA,AMP 或变应原诱导的气道反应性。
T6493 Escitalopram Oxalate

草酸右旋西酞普兰,依他普仑草酸盐,Cipralex,(S)-(+)Citalopram oxalate

Others; 5-HT Receptor; Serotonin Transporter GPCR/G Protein; Neuroscience; Others
Escitalopram Oxalate ((S)-(+)Citalopram oxalate) 是一种外消旋 Citalopram 的 S-对映体,是一种选择性 5-羟色胺再摄取抑制剂,Ki=0.89 nM,比 R(-)-enantiomer 结合亲和力高 30 倍。它对多巴胺转运体和去甲肾上腺素转运体均有选择性,是一种研究抑郁症的抗抑郁药。
T4620 Siramesine

西拉美新,Lu 28-179

Sigma receptor GPCR/G Protein
Siramesine (Lu 28-179) 是sigma-2受体激动剂,通过线粒体的不稳定溶酶体触发细胞死亡,有强大的抗癌活性。它对 sigma-2 受体具有亚纳摩尔亲和力,IC50为 0.12 nM。它对 sigma-2 受体的选择性是 sigma-1 受体的 140倍,IC50为 17 nM。
T14547 JWG-071

JWG071,JWG 071

ERK; Epigenetic Reader Domain Chromatin/Epigenetic; MAPK
JWG-071 是首次报道的 ERK5 激酶选择性化学探针,是一种具有1μM BRD4 IC的BET选择性抑制剂,可提高了 ERK5 活性和 BRD4 选择性。
T6940 PHA-767491 hydrochloride

CAY10572,PHA-767491,PHA767491 HCl,CAY-10572 hydrochloride

Apoptosis; GSK-3; CDK Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells
PHA-767491 hydrochloride (CAY-10572 hydrochloride) 是一种Cdc7-Dbf4(DDK)/Cdk9的双重抑制剂,IC50值分别为 10 nM 和 34 nM。
T10277 AL 8697

p38 MAPK MAPK
AL 8697 是一种特异性 p38α MAPK 抑制剂 (IC50 = 6 nM),其特异性是 p38β (IC50 = 82 nM) 的 14 倍,是其他 91 种激酶的 300 倍。 AL 8697 具有抗炎活性。
T2435 EPZ011989

Histone Methyltransferase Chromatin/Epigenetic
EPZ011989是一种高选择性可口服的 EZH2抑制剂,对wt EZH2以及EZH2突变型Ki 值<3nM。
T6286 RGFP966 (E-isomer)

HDAC Chromatin/Epigenetic; DNA Damage/DNA Repair
RGFP966 是一种 HDAC3 抑制剂,IC50 为 0.08 μM,比其他 HDAC 选择性高 200 倍以上。
T19671 AZ31

AZ 31,AZ-31

ATM/ATR DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
AZ31 是一种 ATM 抑制剂,具有有效性、高选择性、和口服活性。AZ31对 ATM 酶、细胞内 ATM 具有抑制作用,IC50 值 分别为<1.2 nM 和 46 nM。AZ31 表现出优异的 ATR 选择性 、PIKK 家族选择性和泛激酶选择性。AZ31 是一种强效的体外放射增敏剂,可用于研究癌症。
T6064 UK-383367

UK 383367

Procollagen C Proteinase Metabolism
UK-383367 是一种有效、选择性的 BMP-1 抑制剂,IC50=44 nM,对其选择性远高于 MMP 1,2,3,9 和 14。
T3049 TPCA-1

GW683965,IKK2 Inhibitor IV,TPCA1

Apoptosis; IκB/IKK; STAT Apoptosis; JAK/STAT signaling; NF-κB; Stem Cells
TPCA-1 (TPCA1) 是一种选择性IKK-2抑制剂,IC50值为 17.9 nM。它也是反式激活、DNA 结合以及STAT3磷酸化的一种抑制剂。
T6054 GSK256066

PDE Metabolism
GSK256066 是高亲和力的、选择性的PDE4抑制剂,IC50=3.2 pM,被开发用于慢性阻塞性肺病的研究。
T21703 4-Chlorophenylguanidine hydrochloride

Others Others
4-Chlorophenylguanidine hydrochloride 是一种有效的尿激酶选择性抑制剂。
T26109 Robenacoxib

Onsior

COX Immunology/Inflammation; Neuroscience
Robenacoxib (Onsior) 是一种对环氧化酶-2 有很强的选择性的非甾体化合物,具有抗炎活性。
T19917 Gepirone

5-HT Receptor GPCR/G Protein; Neuroscience
Gepirone 属于丁螺环酮家族的 5-HT1A 受体激动剂。它对 5-HT1A 受体的选择性高于 SSRIs。
T22990 ML-090

Fluoflavine

NADPH-oxidase; Others Immunology/Inflammation; Others
ML-090 是 NOX1 特异性抑制剂 (IC50 = 90 nM),对 NOX1 的特异性高于 NOX2、NOX3、NOX4(所有 IC50 > 10 μM)100倍。
T1830 BX795

IκB/IKK; Chk; CDK; c-Kit; PDK; Autophagy Autophagy; Cell Cycle/Checkpoint; NF-κB; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
BX795 是一种选择性PDK1抑制剂,也是相对特异性的TBK1和IKKɛ 抑制剂。它抑制 S6K1,Akt,PKCδ 和 GSK3β 的磷酸化,可调节自噬。
T39573 GSK251

PI3K PI3K/Akt/mTOR signaling
GSK251是一种新型的,口服生物利用度高的PI3Kδ抑制剂,具有高效性和高选择性,且具有独特的结合模式。
T36287 Pirtobrutinib

BTK Angiogenesis; Tyrosine Kinase/Adaptors
Pirtobrutinib (LOXO-305) is an advanced BTK inhibitor that displays high selectivity and operates through a non-covalent mechanism. This compound effectively inhibits various BTK C481 substitution mutations, leading to tumor regression in BTK-dependent lymphoma tumors in mouse xenograft models. Furthermore, Pirtobrutinib exhibits remarkable selectivity for BTK, with more than a 300-fold difference compared to 370 other kinases tested. Notably, at a concentration of 1 μM, Pirtobrutinib demonstrat...
T16936 SS-208

HDAC Chromatin/Epigenetic; DNA Damage/DNA Repair
SS-208 是一种选择性的 HDAC6 抑制剂 (IC50 = 12 nM),具有抗肿瘤活性。 SS-208 显示出对其他 HDAC 亚型的选择性。
T6306 Erteberel

LY500307

Estrogen Receptor/ERR; Estrogen/progestogen Receptor Endocrinology/Hormones
Erteberel (LY500307) 是一种选择性的雌激素受体 β(ERβ) 激动剂,其Ki=1.54 nM,EC50=3.61 nM。具有抗肿瘤作用。
T8651 CAL-101

(S)-2-(1-(9H-Purin-6-ylamino)ethyl)-5-fluoro-3-phenylquinazolin-4(3H)-one,GS-1101,Idelalisib

PI3K PI3K/Akt/mTOR signaling
CAL-101 (Idelalisib) 是 p110δ 的选择性抑制剂(IC50:2.5 nM;在无细胞试验中);显示对 p110δ 的选择性比 p110α/β/γ 高 40 到 300 倍,对 p110δ 的选择性比 C2β、hVPS34、DNA-PK 和 mTOR 高 400 到 4000 倍。
T6378 AMG-458

AMG 458

c-Met/HGFR Tyrosine Kinase/Adaptors
AMG-458 是一种口服有活力的c-Met 选择性抑制剂,其对人和小鼠的Ki 分别为 1.2 nM 和 2.0 nM。
T68134 Ro-3201195

p38 MAPK MAPK
Ro-3201195是一种新型可口服的p38 MAPK 抑制剂,具有很高的选择性。
T6757 AMG319

PI3K PI3K/Akt/mTOR signaling
AMG319 是一种PI3Kδ选择性抑制剂,其 IC50=18 nM。
T16777 ROC-325

Apoptosis; Autophagy Apoptosis; Autophagy
ROC-325 是一种有效的口服活性自噬抑制剂,具有抗癌活性。 ROC-325 诱导肾细胞癌凋亡并表现出良好的特异性。
T6358 1-Azakenpaullone

1-氮杂坎帕罗酮,azakenpaullone

GSK-3 PI3K/Akt/mTOR signaling; Stem Cells
1-Azakenpaullone (azakenpaullone) 是一种 ATP 竞争性的、具有高度选择性的糖原合成酶激酶3 β (GSK-3β)的抑制剂,其 IC50=18 nM。
T36631 BAY-6035

MEK; Histone Methyltransferase Chromatin/Epigenetic; MAPK
BAY-6035 是 SET 和 MYND 结构域蛋白 3 (SMYD3) 的抑制剂。 BAY-6035 的选择性比其他组蛋白甲基转移酶高 100 倍以上。
T23602 ABC99

ABC 99,ABC-99

Wnt/beta-catenin Cytoskeletal Signaling; Stem Cells
ABC99是 wnt 脱酰基酶的一种选择性不可逆抑制剂。ABC99抑制 NOTUM(IC50:13 nM)。它还显示了对丝氨酸水解酶家族的优良选择性。
T6578 ME0328

PARP Chromatin/Epigenetic; DNA Damage/DNA Repair
ME0328 是一种有效的选择性 PARP 抑制剂,对 PARP3 的 IC50 为 0.89 μM。
T6303L CCT128930 hydrochloride

CCT128930 hydrochloride(885499-61-6 Free base)

Apoptosis; Akt; PKA; mTOR; Autophagy Apoptosis; Autophagy; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
CCT128930 hydrochloride (CCT128930 hydrochloride) 是一种选择性 AKT 抑制剂,具有抗肿瘤活性。它通过靶向 AKT 的 Met282 (PKA-AKT 嵌合体的 Met173),对 PKA 激酶具有 28 倍的选择性,对 p70S6K 具有 20 倍的选择性。
T36244 SJF 1521

Others Others
Selective EGFR Degrader. Comprises the EGFR inhibitor lapatinib (Cat. No. 6811) joined by a linker to a von Hippel-Lindau (VHL) recruiting ligand. Exhibits selectivity for EGFR, including mutant forms, over HER2. Induces degradation of EGFR in OVCAR8 cells.
TP1975L [Ala11,D-Leu15]-Orexin B acetate

[Ala11,D-Leu15]-Orexin B acetate (532932-99-3 Free base)

OX Receptor GPCR/G Protein; Neuroscience
[Ala11,D-Leu15]-Orexin B acetate 是一种特异性 orexin-2 受体 (OX2) 激动剂,EC50 为 0.13 nM,比 OX1 (52 nM) 特异性高 400 倍。
T5503 IPSU

OX Receptor GPCR/G Protein; Neuroscience
IPSU 是可口服和脑渗透性的选择性OX2R 拮抗剂,pKi 值为7.85。
T22114 NESS 0327

Cannabinoid Receptor GPCR/G Protein
NESS 0327 是一种高选择性大麻素 CB1 受体拮抗剂。
T4637 R-7050

TNF-α Antagonist III

TNF Apoptosis
R-7050 (TNF-α Antagonist III) 是一种肿瘤坏死因子受体拮抗剂,对 TNFα具有更高选择性。
T2356 Ro-3306

Apoptosis; ERK; SGK; PKA; CDK; PKC Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; MAPK; Metabolism; Tyrosine Kinase/Adaptors
Ro 3306 是一种 CDK1 抑制剂,可以抑制 CDK1、CDK1/cyclin B1 和 CDK2/cyclin E (Ki=20/35/340 nM),具有选择性和 ATP 竞争性。Ro-3306 具有抗肿瘤活性,可以抑制细胞周期阻滞,诱导细胞凋亡。

化合物

Stafia-1
Cat.No: T9339
Synonym:
Target: STAT
MBM-55
Cat.No: T11960
Synonym:
Target: GSK-3, MAPK, DYRK, Akt, Chk, Bcr-Abl, CDK, S6 Kinase, Aurora Kinase
HPK1-IN-7
Cat.No: T9470
Synonym:
Target: MAPK
Desmethyl-VS-5584
Cat.No: T4199
Synonym:
Target: PI3K, mTOR
PDE9-IN-(S)-C33
Cat.No: T28352
Synonym: (S)-C33
Target: PDE
GSK620
Cat.No: T9020
Synonym:
Target: Epigenetic Reader Domain
Ivachtin
Cat.No: T11696
Synonym: Caspase-3 Inhibitor VII
Target: Caspase
RVX-297
Cat.No: T28628
Synonym: RVX297
Target: Epigenetic Reader Domain
SAR-020106
Cat.No: T21331
Synonym:
Target: Chk
BI-1347
Cat.No: T5405
Synonym:
Target: CDK
IRE1α kinase-IN-1
Cat.No: T9564
Synonym:
Target: IRE1
Siramesine hydrochloride
Cat.No: T1885
Synonym: Lu 28-179 hydrochloride,西拉美新盐酸盐
Target: Ferroptosis, Sigma receptor, lysosomal autophagy
SB-408124
Cat.No: T6658
Synonym: N-(6,8-二氟-2-甲基-4-喹啉)- N-[4-(二甲氨基)苯基]尿素
Target: OX Receptor
GS-6201
Cat.No: T15418
Synonym: CVT-6883
Target: Adenosine Receptor
Escitalopram Oxalate
Cat.No: T6493
Synonym: 草酸右旋西酞普兰,依他普仑草酸盐,Cipralex,(S)-(+)Citalopram oxalate
Target: Others, 5-HT Receptor, Serotonin Transporter
Siramesine
Cat.No: T4620
Synonym: 西拉美新,Lu 28-179
Target: Sigma receptor
JWG-071
Cat.No: T14547
Synonym: JWG071,JWG 071
Target: ERK, Epigenetic Reader Domain
PHA-767491 hydrochloride
Cat.No: T6940
Synonym: CAY10572,PHA-767491,PHA767491 HCl,CAY-10572 hydrochloride
Target: Apoptosis, GSK-3, CDK
AL 8697
Cat.No: T10277
Synonym:
Target: p38 MAPK
EPZ011989
Cat.No: T2435
Synonym:
Target: Histone Methyltransferase
RGFP966 (E-isomer)
Cat.No: T6286
Synonym:
Target: HDAC
AZ31
Cat.No: T19671
Synonym: AZ 31,AZ-31
Target: ATM/ATR
UK-383367
Cat.No: T6064
Synonym: UK 383367
Target: Procollagen C Proteinase
TPCA-1
Cat.No: T3049
Synonym: GW683965,IKK2 Inhibitor IV,TPCA1
Target: Apoptosis, IκB/IKK, STAT
GSK256066
Cat.No: T6054
Synonym:
Target: PDE
4-Chlorophenylguanidine hydrochloride
Cat.No: T21703
Synonym:
Target: Others
Robenacoxib
Cat.No: T26109
Synonym: Onsior
Target: COX
Gepirone
Cat.No: T19917
Synonym:
Target: 5-HT Receptor
ML-090
Cat.No: T22990
Synonym: Fluoflavine
Target: NADPH-oxidase, Others
BX795
Cat.No: T1830
Synonym:
Target: IκB/IKK, Chk, CDK, c-Kit, PDK, Autophagy
GSK251
Cat.No: T39573
Synonym:
Target: PI3K
Pirtobrutinib
Cat.No: T36287
Synonym:
Target: BTK
SS-208
Cat.No: T16936
Synonym:
Target: HDAC
Erteberel
Cat.No: T6306
Synonym: LY500307
Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor
CAL-101
Cat.No: T8651
Synonym: (S)-2-(1-(9H-Purin-6-ylamino)ethyl)-5-fluoro-3-phenylquinazolin-4(3H)-one,GS-1101,Idelalisib
Target: PI3K
AMG-458
Cat.No: T6378
Synonym: AMG 458
Target: c-Met/HGFR
Ro-3201195
Cat.No: T68134
Synonym:
Target: p38 MAPK
AMG319
Cat.No: T6757
Synonym:
Target: PI3K
ROC-325
Cat.No: T16777
Synonym:
Target: Apoptosis, Autophagy
1-Azakenpaullone
Cat.No: T6358
Synonym: 1-氮杂坎帕罗酮,azakenpaullone
Target: GSK-3
BAY-6035
Cat.No: T36631
Synonym:
Target: MEK, Histone Methyltransferase
ABC99
Cat.No: T23602
Synonym: ABC 99,ABC-99
Target: Wnt/beta-catenin
ME0328
Cat.No: T6578
Synonym:
Target: PARP
CCT128930 hydrochloride
Cat.No: T6303L
Synonym: CCT128930 hydrochloride(885499-61-6 Free base)
Target: Apoptosis, Akt, PKA, mTOR, Autophagy
SJF 1521
Cat.No: T36244
Synonym:
Target: Others
[Ala11,D-Leu15]-Orexin B acetate
Cat.No: TP1975L
Synonym: [Ala11,D-Leu15]-Orexin B acetate (532932-99-3 Free base)
Target: OX Receptor
IPSU
Cat.No: T5503
Synonym:
Target: OX Receptor
NESS 0327
Cat.No: T22114
Synonym:
Target: Cannabinoid Receptor
R-7050
Cat.No: T4637
Synonym: TNF-α Antagonist III
Target: TNF
Ro-3306
Cat.No: T2356
Synonym:
Target: Apoptosis, ERK, SGK, PKA, CDK, PKC
Cat. No. Product Name Target Signaling Pathways
T0185 Escitalopram

Seroplex,依他普仑,S-(+)-Citalopram,艾司西酞普兰,(S)-Citalopram

Dopamine Receptor; 5-HT Receptor; Serotonin Transporter; Adrenergic Receptor; AChR; Norepinephrine; Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Escitalopram (Seroplex) 是一种外消旋 Citalopram 的 S-对映体,是一种选择性 5-羟色胺再摄取抑制剂,Ki=0.89 nM,比 R(-)-enantiomer 结合亲和力高 30 倍。它对多巴胺转运体和去甲肾上腺素转运体均有选择性,是一种研究抑郁症的抗抑郁药。
T2826 Asaraldehyde

Asarylaldehyde,2,4,5-trimethoxy-Benzaldehyde,Asaronaldehyde,细辛醛

COX Immunology/Inflammation; Neuroscience
Asaraldehyde (2,4,5-trimethoxy-Benzaldehyde) 是COX-2抑制剂,能够明显降低环加氧酶 II (COX-2) 的活性(IC50:100 μg/mL)。
T3S1251 Neoruscogenin

ROR Metabolism
Neoruscogenin 是甾体 sapogenin 家族的成员,是一种可生物利用且具有高亲和力的核受体RORα (NR1F1)激动剂。
T6512 G-418 disulfate

Geneticin,G418 Sulfate,Antibiotic G-418 sulfate,遗传霉素,Geneticin sulfate

Antibacterial; Antibiotic Microbiology/Virology
G-418 disulfate (Geneticin sulfate) 属于氨基糖苷类抗生素,是一种蛋白质合成的抑制剂,具有真核细胞选择性。G-418 disulfate 通过抑制肽链的延伸来阻断多肽合成。
T7472 7-Hydroxyflavone

7-羟基黄酮,7羟基黄酮

P450 Metabolism
7-Hydroxyflavone 是一种黄酮类化合物,从M. indica 中分离得到,具有抗炎活性。它利用 ERK/Nrf2/HO-1 通路保护肾细胞,使其免受尼古丁诱导的细胞毒性。
T0665 Xanthine

2,6-Dihydroxypurine,海生丁(黄嘌呤),黄嘌呤,Isoxanthine

Endogenous Metabolite; Adenosine Receptor GPCR/G Protein; Metabolism; Neuroscience
Xanthine (Isoxanthine) 是一种植物生物碱,存在于茶、咖啡和可可中。Xanthine 是温和的中枢神经系统激活剂,也是嘌呤降解途径的中间产物。
T11041 Dihydro-β-erythroidine hydrobromide

DHβE hydrobromide

Others Others
Dihydro-β-erythroidine hydrobromide(DHβE) is a potent, oral active and competitive antagonist of neuronal nicotinic acetylcholine receptors (nAChRs). Dihydro-β-carotene hydrobromide showed selectivity to α4β4 and α4β2nAChR, with IC50 of 0.19 and 0.37 μM,
T74005 Urolithin D

Others Others
Urolithin D 是EphA 受体的竞争性可逆拮抗剂。Urolithin D 表现出类内选择性。
TN4788 Pierreione B

mTOR PI3K/Akt/mTOR signaling
Pierreione B is an inhibitor of mTOR signaling with strong anticancer activity. Pierreione A and Pierreione B demonstrate solid tumor selectivity with minimal cytotoxicity.
TN1852 Lancifodilactone F

披针叶五味子二内酯 F

HIV Protease Microbiology/Virology; Proteases/Proteasome
Lancifodilactone F exerts minimal cytotoxicity against C8166 cells (CC50 > 200 microg/mL) and shows anti-HIV activity with EC50 = 20.69 +/- 3.31 microg/mL and a selectivity index > 6.62.
TN3428 Aphadilactone C

Others Others
Aphadilactone C shows significant antimalarial activity with the IC50 value of 170 ± 10 nM. It shows potent and selective inhibition against the diacylglycerol O-acyltransferase-1 (DGAT-1) enzyme (IC50 = 0.46 ± 0.09 uM, selectivity index > 217).
T36303 Psammaplin A

Others Others
Psammaplin A, a marine metabolite, functions as a robust inhibitor of HDAC and DNA methyltransferases, displaying notable potency and selectivity as a DAC1 inhibitor, with an IC50 value of 0.9 nM. It exhibits antimicrobial effects against Gram-positive bacteria and inhibits both DNA synthesis and DNA gyrase activity, also demonstrating antitumor activity[1][2].
T75651 Rivulariapeptolides 988

Others Others
Rivulariapeptolides 988作为一种高效选择性丝氨酸蛋白酶抑制剂,对胰凝蛋白酶、弹性蛋白酶和蛋白酶K的IC50分别为95.46 nM、15.29 nM和85.50 nM。
TN7391 Caffeoylcalleryanin

Others Others
Caffeoylcalleryanin demonstrated potent inhibitory activity against 15-lipoxygenase (15-LOX), with an IC50 value of 1.59 μM. Furthermore, ethanol extract from A. pulchra leaves (EEAPL) was found to contain compounds exhibiting antiviral properties, particularly effective against Dengue virus type 2 (DENV-2). Among these compounds, Caffeoylcalleryanin emerged as the most potent anti-DENV-2 agent, achieving a selectivity index (SI) of 20.0.
T72802 Spongionellol A

Others Others
Spongionellol A 是一种 MDR1(p-糖蛋白) 抑制剂。Spongionellol A 通过诱导 caspase 依赖性的凋亡 (apoptosis) 而对前列腺癌细胞具有较强的细胞毒活性和选择性。Spongionellol A 可用于癌症的研究,如前列腺癌。
T75630 Ganoderic acid Mf

Others Others
Ganoderic acid Mf为具有抗肿瘤活性的三萜类化合物,能导致细胞周期在G1期停滞,并在正常细胞与癌细胞中显示高度选择性,通过线粒体介导途径促进细胞凋亡(apoptosis)。
T73072 PTP1B-IN-20

Others Others
PTP1B-IN-20 是蛋白酪氨酸磷酸酶 1B (PTP1B) 的选择性抑制剂 (IC50=1.05 μM),抑制力超出高度同源 T 细胞蛋白酪氨酸磷酸酶 (TCPTP;IC50=78.0 μM),PTP1B 是抑制 2 型糖尿病的重要靶点。
T79975 Dihydrodehydrodiconiferyl alcohol 9-O-α-L-rhamnopyranoside

HBV Microbiology/Virology
Dihydrodehydrodiconiferyl alcohol 9-O-α-L-rhamnopyranoside(化合物1)是一种具有抗HBV活性的木脂素类化合物。该化合物对HBV表面抗原(HBsAg)的IC50为0.58 mM,而对HBV e抗原(HBeAg)的IC50 > 2.4 mM。其可从八角茴香中提取分离。
T82031 Isoguaiacin

Isoguaiacin为一种天然产物,具有复杂的多环化合物结构,广泛应用于生物医药研究领域。
T75436 Jatrorrhizine hydroxide

Others Others
Jatrorrhizine hydroxide, 一种从黄连中提取的生物碱,展现了神经保护、抗菌、抗疟原虫及抗氧化的活性。作为一种高效的乙酰胆碱酯酶(AChE)抑制剂(IC50=872 nM),其对BuChE的选择性高达115倍。此外,Jatrorrhizine hydroxide还能通过抑制uptake-2 transporter活性来减少血清素(5-HT)和去甲肾上腺素(NE)的摄取,表现出口服活性。
T83913 Mitraciliatine

Others Others
Mitraciliatine是一种在M. speciosa(泰国称为Kratom)中发现的生物碱,是μ-阿片受体(MOR)部分激动剂和κ-阿片受体(KOR)激动剂。该化合物对MOR和KOR具有选择性,与δ-阿片受体(DOR; EC50s分别为228, 218, 和 >1,000 nM,针对小鼠受体在GTPγS结合实验中的表现)。Mitraciliatine(100 nmol/动物,脑室内注射)在小鼠的热水尾部缩回实验中延长了撤回潜伏期,这一效果可以通过敲除MOR而非KOR来逆转。与吗啡不同,Mitraciliatine不会诱发过度活动或呼吸抑制。
T37876 Fengycin

Others Others
Fengycin is a cyclic lipopeptide used as an agricultural fungicide. Fengmycin has an anti-fungal infection effect by damaging the target’s cell membrane[1]. [1]. Sreyoshi Sur, et al. Selectivity and Mechanism of Fengycin, an Antimicrobial Lipopeptide, from Molecular Dynamics. J Phys Chem B. 2018 Mar 1;122(8):2219-2226.

天然产物

Escitalopram
Cat.No: T0185
Synonym: Seroplex,依他普仑,S-(+)-Citalopram,艾司西酞普兰,(S)-Citalopram
Target: Dopamine Receptor, 5-HT Receptor, Serotonin Transporter, Adrenergic Receptor, AChR, Norepinephrine, Histamine Receptor
Asaraldehyde
Cat.No: T2826
Synonym: Asarylaldehyde,2,4,5-trimethoxy-Benzaldehyde,Asaronaldehyde,细辛醛
Target: COX
Neoruscogenin
Cat.No: T3S1251
Synonym:
Target: ROR
G-418 disulfate
Cat.No: T6512
Synonym: Geneticin,G418 Sulfate,Antibiotic G-418 sulfate,遗传霉素,Geneticin sulfate
Target: Antibacterial, Antibiotic
7-Hydroxyflavone
Cat.No: T7472
Synonym: 7-羟基黄酮,7羟基黄酮
Target: P450
Xanthine
Cat.No: T0665
Synonym: 2,6-Dihydroxypurine,海生丁(黄嘌呤),黄嘌呤,Isoxanthine
Target: Endogenous Metabolite, Adenosine Receptor
Dihydro-β-erythroidine hydrobromide
Cat.No: T11041
Synonym: DHβE hydrobromide
Target: Others
Urolithin D
Cat.No: T74005
Synonym:
Target: Others
Pierreione B
Cat.No: TN4788
Synonym:
Target: mTOR
Lancifodilactone F
Cat.No: TN1852
Synonym: 披针叶五味子二内酯 F
Target: HIV Protease
Aphadilactone C
Cat.No: TN3428
Synonym:
Target: Others
Psammaplin A
Cat.No: T36303
Synonym:
Target: Others
Rivulariapeptolides 988
Cat.No: T75651
Synonym:
Target: Others
Caffeoylcalleryanin
Cat.No: TN7391
Synonym:
Target: Others
Spongionellol A
Cat.No: T72802
Synonym:
Target: Others
Ganoderic acid Mf
Cat.No: T75630
Synonym:
Target: Others
PTP1B-IN-20
Cat.No: T73072
Synonym:
Target: Others
Dihydrodehydrodiconiferyl alcohol 9-O-α-L-rhamnopyranoside
Cat.No: T79975
Synonym:
Target: HBV
Isoguaiacin
Cat.No: T82031
Synonym:
Target:
Jatrorrhizine hydroxide
Cat.No: T75436
Synonym:
Target: Others
Mitraciliatine
Cat.No: T83913
Synonym:
Target: Others
Fengycin
Cat.No: T37876
Synonym:
Target: Others
Cat. No. Product Name Species Expression System
TMPJ-00922 DCK Protein, Human, Recombinant (His & T7)

DCK,Deoxycytidine Kinase

Human E. coli
Deoxycytidine Kinase (DCK) is a member of the DCK/DGK family. DCK exists as a homodimer and is localized to the nucleus. DCK is required for the phosphorylation of the deoxyribonucleosides deoxycytidine (dC), deoxyguanosine (dG), and deoxyadenosine (dA). DCK has broad substrate specificity, and does not display selectivity based on the chirality of the substrate. In addition, DCK is also an essential enzyme for the phosphorylation of numerous nucleoside analogs widely employed as antiviral and c...
TMPJ-01001 CCL11 Protein, Human, Recombinant

SCYA11,C-C Motif Chemokine 11,Eosinophil Chemotactic Protein...

Human E. coli
C-C Motif Chemokine 11 (CCL11) is a secreted protein that belongs to the intercrine beta (chemokine CC) family. In response to the presence of allergens, CCL11 selectively recruits eosinophils, a prominent feature of allergic inflammatory reactions. The effects of CCL11 are mediated by its binding to a G-protein-linked receptor known as a chemokine receptor. Chemokine receptors for CCL11 include CCR2, CCR3 and CCR5. However, it has been found that CCL11 has high degree selectivity for its recept...
TMPH-02301 VPS35 Protein, Human, Recombinant (His & Myc)

VPS35,Vacuolar protein sorting-associated protein 35,Vesicle...

Human E. coli
Acts as component of the retromer cargo-selective complex (CSC). The CSC is believed to be the core functional component of retromer or respective retromer complex variants acting to prevent missorting of selected transmembrane cargo proteins into the lysosomal degradation pathway. The recruitment of the CSC to the endosomal membrane involves RAB7A and SNX3. The CSC seems to associate with the cytoplasmic domain of cargo proteins predominantly via VPS35; however, these interactions seem to be of...

重组蛋白

DCK Protein, Human, Recombinant (His & T7)
Cat.No: TMPJ-00922
Species: Human
Expression System: E. coli
CCL11 Protein, Human, Recombinant
Cat.No: TMPJ-01001
Species: Human
Expression System: E. coli
VPS35 Protein, Human, Recombinant (His & Myc)
Cat.No: TMPH-02301
Species: Human
Expression System: E. coli
Cat. No. Product Name Target Signaling Pathways
T33410 MitoNeoD

Mito Neo D,Mito-Neo-D,Mito Neo-D,Mito-NeoD

MitoNeoD is a novel mitochondria-targeted O2(⋅−) probe that can be used in vivo. It prevents DNA intercalation. MitoNeoD incorporates a carbon-deuterium bond, and enhances O2(⋅−) selectivity.
TMIJ-0242 Tandospirone-d8

Tandospirone-d8 是 Tandospirone 的氘代化合物。Tandospirone 的 CAS 号为 87760-53-0。
TMIJ-0073 Dapoxetine hydrochloride-d7

Dapoxetine hydrochloride-d7 是 Dapoxetine hydrochloride 的氘代化合物。Dapoxetine hydrochloride 的 CAS 号为 129938-20-1。Dapoxetine HCl 是一种具有口服活性的、选择性的血清素再摄取 (serotonin reuptake) 抑制剂 (SSRI),可用于研究早泄 (PE) 。
TMIJ-0235 rac-Tolterodine-d14 Tartrate

rac-Tolterodine-d14 Tartrate 是 rac-Tolterodine Tartrate 的氘代化合物。rac-Tolterodine Tartrate 的 CAS 号为 124937-52-6。Tolterodine Tartrate 是毒蕈碱受体的有效拮抗剂。 它在体内显示出对膀胱和唾液腺的选择性。
TMIH-0461 Prucalopride-13C-d3

Prucalopride-13C-d3 是 Prucalopride 的 13C 和氘代化合物。Prucalopride 的 CAS 号为 179474-81-8。Prucalopride 是一种选择性、高亲和力的 5-HT4A/4B 受体激动剂,Ki为2.5和 8 nM。它对 5-HT4A/4B 受体的选择性是其他 5-HT 受体亚型的 290 倍以上。
TMIH-0235 Finerenone-d5

Finerenone-d5 是 Finerenone 的氘代化合物。Finerenone 的 CAS 号为 1050477-31-0。Finerenone 是一种选择性、具有口服活性的、非甾体类盐皮质激素受体拮抗剂 (IC50=18 nM)。与糖皮质激素受体、雄激素受体和孕酮受体相比,它表现出良好的选择性 (>500-fold)。它在心肾疾病研究中具有潜在的应用前景,如 2 型糖尿病和慢性肾脏疾病。

同位素标记化合物

MitoNeoD
Cat.No: T33410
Synonym: Mito Neo D,Mito-Neo-D,Mito Neo-D,Mito-NeoD
Target:
Tandospirone-d8
Cat.No: TMIJ-0242
Synonym:
Target:
Dapoxetine hydrochloride-d7
Cat.No: TMIJ-0073
Synonym:
Target:
rac-Tolterodine-d14 Tartrate
Cat.No: TMIJ-0235
Synonym:
Target:
Prucalopride-13C-d3
Cat.No: TMIH-0461
Synonym:
Target:
Finerenone-d5
Cat.No: TMIH-0235
Synonym:
Target:
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