ROCK2 Selective Inhibitors

Catalog No.	Product Name	Information	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)	Belumosudil (KD025, SLx-2119) is an orally available, and selective ROCK2 inhibitor with IC50 and K_i of 60 nM and 41 nM, respectively. Phase 2.	Selective	ROCK2, IC50: 60 nM; ROCK2, Ki: 41 nM
S1573	Fasudil HCl	Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.	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
S7563	AT13148	AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1.	Pan	ROCK2, IC50: 4 nM
S7687	GSK269962A HCl	GSK269962A HCl (GSK269962B, GSK269962) is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.	Pan	ROCK2, IC50: 4 nM
S7195	RKI-1447	RKI-1447 is a potent inhibitor of ROCK1 and ROCK2, with IC50 of 14.5 nM and 6.2 nM, respectively, has anti-invasive and antitumor activities.	Pan	ROCK2, IC50: 6.2 nM
S7995	Ripasudil hydrochloride dihydrate	Ripasudil hydrochloride dihydrate is a potent ROCK inhibitor with IC50 of 51 nM and 19 nM for ROCK1 and ROCK2, respectively, used for the treatment of glaucoma and ocular hypertension.	Pan	ROCK2, IC50: 19 nM
S1474	GSK429286A	GSK429286A (RHO-15) is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.	Pan	ROCK2, IC50: 63 nM
S1049	Y-27632 2HCl	Y-27632 2HCl is a selective ROCK1 and ROCK2 inhibitor with a K_i of 140 nM and 300nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.	Pan	ROCK2, Ki: 300 nM
S6390	Y-27632	Y-27632 is a selective ROCK1 and ROCK2 inhibitor with a Ki of 140 nM and 300nM in a cell-free assay, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.	Pan	ROCK2, Ki: 300 nM
S8208	Hydroxyfasudil (HA-1100) HCl	Hydroxyfasudil (HA-1100), an active metabolite of fasudil hydrochloride, is a specific Rho-kinase(ROCK) inhibitor with IC50 values of 0.73 μM and 0.72 μM for ROCK1 and ROCK2, respectively.	Pan	ROCK2, IC50: 0.72 μM