ROCK2 选择性抑制剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S6214 H-1152 dihydrochloride

H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively.

Selective ROCK2, IC50: 0.0120 μM
S7936 Belumosudil (KD025)

KD025是一个具有口服活性,选择性的ROCK2抑制剂,其IC50Ki分别为60 nM和41 nM。Phase 2。

Selective ROCK2, Ki: 41 nM; ROCK2, IC50: 60 nM
S1573 Fasudil (HA-1077) HCl

Fasudil(HA-1077)是一种有效的、具有选择性的Rho抑制剂(ROCK2, Ki=0.33 μM),同时对PKA、PKG、PKC和MLCK也具有抑制活性,Ki值分别为1.6 μM、1.6 μM、3.3 μM、36 μM。

Selective ROCK2, Ki: 330 nM
S6636 Azaindole 1 (TC-S 7001)

Azaindole 1 (TC-S 7001) is a selective Rho-associated protein kinase (ROCK) inhibitor with IC50 of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2 in an ATP-competitive manner.

Pan ROCK2, IC50: 1.1 nM
S7687 GSK269962A HCl

GSK269962是选择性的ROCK(Rho-associated protein kinase)抑制剂,对ROCK1和ROCK2的IC50分别为1.6 nM和4 nM。

Pan ROCK2, IC50: 4 nM
S7563 AT13148

AT13148是一种口服的,ATP竞争性的,多AGC kinase抑制剂,对Akt1/2/3p70S6KPKA,和ROCKI/IIIC50分别为38 nM/402 nM/50 nM,8 nM,3 nM,和6 nM/4 nM。Phase 1。

Pan ROCK2, IC50: 4 nM
S7195 RKI-1447

RKI-1447是一种有效的ROCK1ROCK2抑制剂,IC50分别为14.5 nM和6.2 nM,有抗侵入和抗肿瘤活性。

Pan ROCK2, IC50: 6.2 nM
S7995 Ripasudil (K-115) hydrochloride dihydrate

Ripasudil (K-115) hydrochloride dihydrate是有效的 ROCK 抑制剂,作用于ROCK1 和 ROCK2的 IC50 分别为 51 nM 和 19 nM,用作青光眼和眼内高压的治疗。

Pan ROCK2, IC50: 19 nM
S1474 GSK429286A

GSK429286A是一种选择性的ROCK1ROCK2抑制剂,IC50分别为14 nM和63 nM。

Pan ROCK2, IC50: 63 nM
S6390 Y-27632

Y-27632 is a specific inhibitor of ROCK with an Ki of 140 nM for ROCK1 (p160ROCK). Y-27632 shows >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.

Pan ROCK2, Ki: 300 nM
S1049 Y-27632 2HCl

Y-27632 2HCl是一种选择性ROCK1(p160ROCK)抑制剂,无细胞试验中Ki为140 nM,比对其他激酶包括PKC,cAMP依赖性蛋白激酶,MLCK和PAK的作用强200多倍。

Pan ROCK2, Ki: 300 nM
S8208 Hydroxyfasudil (HA-1100) HCl

Hydroxyfasudil(HA-1100)是fasudil hydrochloride的活性代谢物,是特异性的Rho-kinase(ROCK)抑制剂,对ROCK1ROCK2的IC50分别为0.73 μM和0.72 μM。

Pan ROCK2, IC50: 0.72 μM
S3233 Emetine hydrochloride

Emetine hydrochloride (NSC 33669), a principal alkaloid extracted from the root of ipecac clinically used as an emetic and antiprotozoal drug, reduces HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α), PDK1, RhoA, Rho-kinases (ROCK1 and ROCK2) and BRD4. Emetine hydrochloride inhibits cellular autophagy and has anti-malarial, anti-viral, anti-bacterial and anti-amoebic effect.

Pan