ROCK2 Inhibitor

Y-27632 is a ROCK inhibitor with K_i values of 220 nM and 300 nM for ROCK1 and ROCK2, respectively. Y-27632 exerts anti-inflammatory and immunomodulatory effects in systemic lupus erythematosus models by inhibiting the ROCK/NF-κB pathway. Y-27632 enhances autophagy by inhibiting the AKT/mTOR pathway, thereby inducing apoptosis apoptosis in oral squamous cell carcinoma. Y-27632 induces the formation of tunneling nanotubes in ARPE-19 cells and significantly enhances mitochondrial transfer through these channels. Y-27632 promotes neurite outgrowth in PC12 cells by activating the Rac1/NOX1/ROS/AKT/PAK1 signaling cascade.

Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor (ROCK-I K_i=220 nM; ROCK-II K_i=300 nM). Y-27632 dihydrochloride shows antiepileptic effects.

Chroman 1 is a highly potent and selective ROCK inhibitor. Chroman 1 is more potent against ROCK2 (IC₅₀=1 pM) than ROCK1 (IC₅₀=52 pM). Chroman 1 also has inhibitory activity against MRCK, with an IC₅₀ of 150 nM.

Fasudil (HA-1077; AT877) Hydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an K_i 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. Fasudil Hydrochloride is also a potent Ca²⁺ channel antagonist and vasodilator.

Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC₅₀s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties.

LASSBio-2382 is a dual ROCK1/ROCK2 inhibitor with ROCK1 IC₅₀ of 0.005 μM and ROCK2 IC₅₀ of 0.003 μM. LASSBio-2382 inhibits viability and migration of cancer cells. LASSBio-2382 can be used for the research of triple-negative breast cancer.

ROCK2-IN-17 is an orally active and selective ROCK2 inhibitor with an IC₅₀ of 8.1 nM. ROCK2-IN-17 achieves its antifibrotic effect by inhibiting the TGF-β/Smad and ROCK2/STAT3 signaling pathways. ROCK2-IN-17 can be used for pulmonary fibrosis research.

ROCK2-IN-15 (2-11) is a ROCK2 inhibitor with selective activity against Rho-kinase mediated phosphorylation of myosin light chain phosphates .ROCK2-IN-15 can be used for the research of cardiovascular diseases, pulmonary diseases, inflammatory diseases, neurological diseases, proliferative diseases .

CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC₅₀ of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC₅₀s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure.

GSK269962A (GSK 269962) is a potent ROCK inhibitor with IC₅₀s of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively. GSK269962A has anti-inflammatory and vasodilatory activities.

Fasudil (HA-1077; AT877) is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an K_i 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. Fasudil is also a potent Ca²⁺ channel antagonist and vasodilator.

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

Belumosudil mesylate (KD025 mesylate) is a selective inhibitor of ROCK2 with IC₅₀s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties.

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

ROCK inhibitor-2 (compound 6) is a selective dual inhibitor of ROCK1 and ROCK2, with IC₅₀ values of 160 nM and 21 nM, respectively. ROCK inhibitor-2 inhibits pMYPT1 with IC₅₀ of 75 nM. ROCK inhibitor-2 exhibits antitumor activity.

RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC₅₀ values of 14.5 nM and 6.2 nM, respectively.

SR-3677 is a potent and selective ROCK-II inhibitor with an IC₅₀ of ~3 nM.

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

SAR407899 is a selective, potent and ATP-competitive ROCK inhibitor, with an IC₅₀ of 135 nM for ROCK-2, and K_is of 36 nM and 41 nM for human and rat ROCK-2, respectively. SAR407899 shows stable inhibition of migrasome formation.

CRT0066854 is a potent and selective atypical PKC isoenzymes inhibitor. CRT0066854 is against full-length (FL) PKCι, PKCζ, and ROCK-II kinases with IC₅₀ values of 132 nM, 639 nM, and 620 nM, respectively.