ROCK

信号通路图

研究领域

抑制剂选择性比较

特异性亚型抑制剂

ROCK产品

所有产品 ROCK抑制剂(14)

产品目录	产品描述	文献引用	实验数据
S1049	Y-27632 2HCl Y-27632 2HCl是一种选择性ROCK1(p160ROCK)抑制剂，无细胞试验中K_i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。	Cell, 2019, 179(1):147-164 Cell, 2019, 179(1):147-164 Cell, 2019, 176(5):1158-1173	The Rho GTPase-JNK pathway is required for the inhibitory effects of vandetanib on Calu-6 cells invasion. Calu-6 cells were incubated for 24 h in the presence or absence of vandetanib (1 or 2 uM), SP600125 (50 or 100 uM), and Y27632 (5 or 10 uM). The morphology of the Calu-6 cells was examined under a light microscope. Scale bar: 50 um.
S1459	Thiazovivin Thiazovivin是一种新型ROCK抑制剂，无细胞试验中IC50为0.5 μM，在单细胞分离后，促进人胚胎干细胞（hESC）的存活。	Cell Rep, 2019, 27(2):616-630 J Mol Cell Cardiol, 2019, 134:1-12 J Biol Chem, 2019, 294(37):13657-13670
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。	Sci Signal, 2019, 12(587) J Cereb Blood Flow Metab, 2019, 39(1):58-73 Cell Mol Neurobiol, 2019, 39(5):637-650	The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation.
S1474	GSK429286A GSK429286A是一种选择性的ROCK1和ROCK2抑制剂，IC50分别为14 nM和63 nM。	J Pathol, 2018, 245(4):456-467 Cancer Res, 2017, 77(9):2413-2423 Respir Res, 2017, 18(1):111	ROCK antagonists interfere with infection-induced changes in cell shape, but do not reduce HCMV yield. (A) ROCK antagonists block actin reorganization after infection. Fibroblasts were treated with solvent (DMSO) or drug (10 uM Y27632 or 140 nM GSK429286A) beginning 1 h after mock infection or infection with WT virus. Cells received fresh medium containing solvent or drug every 24 h. Cultures were assayed for actin using labeled phalloidin (red), pUL37 (green), and DNA (blue). (B) ROCK antagonist blocks cell rounding at 24 hpi. Fibroblasts were treated with solvent or drug beginning 1 h after mock infection or infection with WT virus. Cultures received fresh medium with drug every 24 h and were analyzed by treatment with 5 μM fluorophore calcein red-orange AM for 1 h, followed by spinning disk confocal Z-stack live cell imaging and reconstruction of 3D images. (C) ROCK activity does not influence virus yield. Fibroblasts were treated with solvent or ROCK antagonists beginning 1 h after infection with WT HCMV. Cultures received fresh medium with drug every 24 h, and extracellular virus yields were determined by plaque assay.
S7195	RKI-1447 RKI-1447是一种有效的ROCK1和ROCK2抑制剂，IC50分别为14.5 nM和6.2 nM，有抗侵入和抗肿瘤活性。	Neoplasia, 2018, 20(1):44-56 Oncogene, 2017, 36(8):1080-1089 Anticancer Res, 2017, 37(4):1805-1818	(d) ROCK inhibition blocks CC-RCC migration in a transwell assay. RCC10 or 786-O cells were treated with Y-27632, RKI 1447 or DMSO vehicle (as indicated) for 6 h. The assay was performed in duplicate and the experiment was repeated three times. Statistical analysis in (b-d) was performed using a paired t-test comparing each normalized dose to the negative control (P<0.05, P<0.01 and **P<0.001); s.e.m.'s are shown.
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。	Am J Physiol Heart Circ Physiol, 2019, 10.1152/ajpheart.00685.2018
S8226	Netarsudil (AR-13324) 2HCl Netarsudil (AR-13324)是ROCK抑制剂，Ki值为0.2-10.3 nM。目前处于治疗青光眼和高眼压症的临床实验中。
S7935	Y-39983 HCl Y-39983是选择性ROCK抑制剂，IC50为3.6 nM。	In Vitro Cell Dev Biol Anim, 2019, 55(4):260-271
S8448	ZINC00881524 (ROCK inhibitor) ZINC00881524是ROCK抑制剂。	Nature, 2018, 563(7733):701-704 Stem Cells Dev, 2014, 23(17):2119-25 Eur J Obstet Gynecol Reprod Biol, 2014, 183:1-4
S7936	KD025 (SLx-2119) KD025是一个具有口服活性，选择性的ROCK2抑制剂，其IC50和K_i分别为60 nM和41 nM。Phase 2。
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。
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ROCK1和ROCK2的IC50分别为0.73 μM和0.72 μM。
S8489	GSK180736A (GSK180736) GSK180736A是一种Rho相关的、含卷曲螺旋（coiled-coil）的蛋白激酶抑制剂，与GRK2(G protein-coupled receptor kinase 2)结合，logIC50为-6.6。对GRK2的选择性比对GRK1和GRK5高400倍以上。
S7563	AT13148 AT13148是一种口服的，ATP竞争性的，多AGC kinase抑制剂，对Akt1/2/3，p70S6K，PKA，和ROCKI/II的IC50分别为38 nM/402 nM/50 nM，8 nM，3 nM，和6 nM/4 nM。Phase 1。	Cancer Sci, 2016, 107(11):1563-1571 Biochem Biophys Res Commun, 2016, 478(1):330-6	AT13148 exerts cytotoxic and anti-proliferative activity against human gastric cancer cells. Human gastric cancer cells (HGC-27, AGS, SNU-601, N87 and MKN-28 lines) or GEC-1 gastric epithelial cells were treated with applied concentration of AT13148 for indicated time, cell survival (A and E), cell proliferation (B and F), cell cycle distribution (C, for HGC-27 cells) and cell death (D, for HGC-27 cells) were tested by the described assays, separately. Data were presented as mean ± SD. “Ctrl” stands for untreated control cells (For all figures). “hr/hrs” stands for hour/hours (For all figures). Experiments in this figure were repeated for five times. *p < 0.05 vs. “Ctrl” group.

产品目录	产品描述	文献引用	实验数据
S1049	Y-27632 2HCl Y-27632 2HCl是一种选择性ROCK1(p160ROCK)抑制剂，无细胞试验中K_i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。	Cell,2019, 179(1):147-164 Cell,2019, 179(1):147-164 Cell,2019, 176(5):1158-1173	The Rho GTPase-JNK pathway is required for the inhibitory effects of vandetanib on Calu-6 cells invasion. Calu-6 cells were incubated for 24 h in the presence or absence of vandetanib (1 or 2 uM), SP600125 (50 or 100 uM), and Y27632 (5 or 10 uM). The morphology of the Calu-6 cells was examined under a light microscope. Scale bar: 50 um.
S1459	Thiazovivin Thiazovivin是一种新型ROCK抑制剂，无细胞试验中IC50为0.5 μM，在单细胞分离后，促进人胚胎干细胞（hESC）的存活。	Cell Rep,2019, 27(2):616-630 J Mol Cell Cardiol,2019, 134:1-12 J Biol Chem,2019, 294(37):13657-13670
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。	Sci Signal,2019, 12(587) J Cereb Blood Flow Metab,2019, 39(1):58-73 Cell Mol Neurobiol,2019, 39(5):637-650	The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation.
S1474	GSK429286A GSK429286A是一种选择性的ROCK1和ROCK2抑制剂，IC50分别为14 nM和63 nM。	J Pathol,2018, 245(4):456-467 Cancer Res,2017, 77(9):2413-2423 Respir Res,2017, 18(1):111	ROCK antagonists interfere with infection-induced changes in cell shape, but do not reduce HCMV yield. (A) ROCK antagonists block actin reorganization after infection. Fibroblasts were treated with solvent (DMSO) or drug (10 uM Y27632 or 140 nM GSK429286A) beginning 1 h after mock infection or infection with WT virus. Cells received fresh medium containing solvent or drug every 24 h. Cultures were assayed for actin using labeled phalloidin (red), pUL37 (green), and DNA (blue). (B) ROCK antagonist blocks cell rounding at 24 hpi. Fibroblasts were treated with solvent or drug beginning 1 h after mock infection or infection with WT virus. Cultures received fresh medium with drug every 24 h and were analyzed by treatment with 5 μM fluorophore calcein red-orange AM for 1 h, followed by spinning disk confocal Z-stack live cell imaging and reconstruction of 3D images. (C) ROCK activity does not influence virus yield. Fibroblasts were treated with solvent or ROCK antagonists beginning 1 h after infection with WT HCMV. Cultures received fresh medium with drug every 24 h, and extracellular virus yields were determined by plaque assay.
S7195	RKI-1447 RKI-1447是一种有效的ROCK1和ROCK2抑制剂，IC50分别为14.5 nM和6.2 nM，有抗侵入和抗肿瘤活性。	Neoplasia,2018, 20(1):44-56 Oncogene,2017, 36(8):1080-1089 Anticancer Res,2017, 37(4):1805-1818	(d) ROCK inhibition blocks CC-RCC migration in a transwell assay. RCC10 or 786-O cells were treated with Y-27632, RKI 1447 or DMSO vehicle (as indicated) for 6 h. The assay was performed in duplicate and the experiment was repeated three times. Statistical analysis in (b-d) was performed using a paired t-test comparing each normalized dose to the negative control (P<0.05, P<0.01 and **P<0.001); s.e.m.'s are shown.
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。	Am J Physiol Heart Circ Physiol,2019, 10.1152/ajpheart.00685.2018
S8226	Netarsudil (AR-13324) 2HCl Netarsudil (AR-13324)是ROCK抑制剂，Ki值为0.2-10.3 nM。目前处于治疗青光眼和高眼压症的临床实验中。
S7935	Y-39983 HCl Y-39983是选择性ROCK抑制剂，IC50为3.6 nM。	In Vitro Cell Dev Biol Anim,2019, 55(4):260-271
S8448	ZINC00881524 (ROCK inhibitor) ZINC00881524是ROCK抑制剂。	Nature,2018, 563(7733):701-704 Stem Cells Dev,2014, 23(17):2119-25 Eur J Obstet Gynecol Reprod Biol,2014, 183:1-4
S7936	KD025 (SLx-2119) KD025是一个具有口服活性，选择性的ROCK2抑制剂，其IC50和K_i分别为60 nM和41 nM。Phase 2。
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。
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ROCK1和ROCK2的IC50分别为0.73 μM和0.72 μM。
S8489	GSK180736A (GSK180736) GSK180736A是一种Rho相关的、含卷曲螺旋（coiled-coil）的蛋白激酶抑制剂，与GRK2(G protein-coupled receptor kinase 2)结合，logIC50为-6.6。对GRK2的选择性比对GRK1和GRK5高400倍以上。
S7563	AT13148 AT13148是一种口服的，ATP竞争性的，多AGC kinase抑制剂，对Akt1/2/3，p70S6K，PKA，和ROCKI/II的IC50分别为38 nM/402 nM/50 nM，8 nM，3 nM，和6 nM/4 nM。Phase 1。	Cancer Sci,2016, 107(11):1563-1571 Biochem Biophys Res Commun,2016, 478(1):330-6	AT13148 exerts cytotoxic and anti-proliferative activity against human gastric cancer cells. Human gastric cancer cells (HGC-27, AGS, SNU-601, N87 and MKN-28 lines) or GEC-1 gastric epithelial cells were treated with applied concentration of AT13148 for indicated time, cell survival (A and E), cell proliferation (B and F), cell cycle distribution (C, for HGC-27 cells) and cell death (D, for HGC-27 cells) were tested by the described assays, separately. Data were presented as mean ± SD. “Ctrl” stands for untreated control cells (For all figures). “hr/hrs” stands for hour/hours (For all figures). Experiments in this figure were repeated for five times. *p < 0.05 vs. “Ctrl” group.

Tags: ROCK inhibition | ROCK activity | ROCK activation | Rho kinase inhibition | Rho kinase activation | Rho kinase activity | ROCK phosphorylation | ROCK signaling pathway | Rho kinase assay | Rho kinase signaling pathway | ROCK inhibitors for glaucoma | ROCK inhibitor review