ROCK

ROCK2-IN-2 is a selective ROCK2 inhibitor extracted from patent US20180093978A1, Compound A-30, has an IC50 of <1 μM.

ROCK-IN-1 is a potent inhibitor of ROCK, with an IC50 of 1.2 nM for ROCK2.

BDP5290 is a potent inhibitor of ROCK and MRCK with IC50 values of 17nM, 230nM, 123nM and 100nM for MRCKβ, ROCK1, ROCK2, respectively.

A ROCK inhibitor

Rho-Kinase-IN-1 is a Rho kinase (ROCK) inhibitor (Ki values of 30.5 and 3.9 nM for ROCK1 and ROCK2, respectively) extracted from US20090325960A1, compound 1.008.

Azaindole 1 (Azaindole 1; TC-S 7001) is an orally active and ATP-competitive ROCK inhibitor with IC50s of 0.6 and 1.1nM for human ROCK-1 and ROCK-2, respectively.

H-1152 is a membrane-permeable and selective ROCK inhibitor, with a Ki value of 1.6 nM, and an IC50 value of 12 nM for ROCK2.

H-1152 dihydrochloride is a membrane-permeable and selective ROCK inhibitor, with a Ki value of 1.6 nM, and an IC50 value of 12 nM for ROCK2.

Ripasudil free base (K-115 free base) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.

ROCK inhibitor-2 is a selective Rho kinase (ROCK) inhibitor with IC 50 values of 17nM and 2nM for ROCK1 and ROCK2, respectively, and has anti-tumor activity.

Y-33075 is a potent ROCK (Rho-associated protein kinase) inhibitor with an IC 50 value of 3.6nM.

GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM).

CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis.

Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability.

Afuresertib is a selective, orally bioavailable inhibitor of Akt1, 2, and 3 with Ki values of 0.08, 2, and 2.6 nM, respectively.

Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability.

CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of G protein-coupled receptor kinase 2 (GRK2) and GRK3 (IC 50 s=18 and 5.4nM, respectively).

Fasudil (HA-1077; AT877) dihydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. HA-1077 (hydrochloride) is also a potent Ca2+ channel antagonist and vasodilator.

LX7101 is a potent inhibitor of LIM kinase (LIMK) 1 and 2 and Rho-associated kinase 1 (ROCK-1) and ROCK-2 with IC50 values of 32, 4.3, 69, and 32 nM, respectively.

A ROCK1 and ROCK2 inhibitor

A ROCK2 inhibitor