ROCK2 Selective Inhibitors

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S7936 Belumosudil (KD025)

Belumosudil (KD025, SLx-2119) is an orally available, and selective ROCK2 inhibitor with IC50 and Ki of 60 nM and 41 nM, respectively. Phase 2.

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

Fasudil (HA-1077, AT-877), 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
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
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
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 (K-115) hydrochloride dihydrate

Ripasudil (K-115) hydrochloride dihydrate is 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 (p160ROCK) inhibitor with Ki of 140 nM 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