ROCK1 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.

LASSBio-2389 is a selective ROCK2 inhibitor with an IC₅₀ of 0.051 μM and an IC₅₀ of 1.143 μM against ROCK1. LASSBio-2389 reduces the viability of MDA-MB-231 cells and inhibits cell migration. LASSBio-2389 is applicable to the research of triple-negative breast cancer.

RX-044 is a ROCK1/ROCK2 inhibitor with ROCK1 IC₅₀ 10.01 nM and ROCK2 IC₅₀ 9.68 nM, and demonstrates kinase selectivity. RX-044 induces reversible cell retraction, modulates cytoskeletal organization via F-actin depolymerization, inhibits cell contractility, and attenuates TGF-β2-induced cell migration. RX-044 preserves retinal ganglion cell survival, restores electroretinography responses, and ameliorates histopathological changes. RX-044 lowers intraocular pressure in a mouse ocular hypertension model. RX-044 shows no cytotoxicity in target cells. RX-044 exhibits initial ocular irritation that subsides with extended dosing. RX-044 can be used for the research of glaucoma.

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.

GSK429286A is a selective inhibitor of ROCK1 with an IC₅₀ value of 14 nM.

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.

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.

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.

BAY-549 (Azaindole 1), a chemical probe, is an orally active and ATP-competitive ROCK inhibitor with IC₅₀s of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2, respectively.

AT13148 is an orally active and ATP-competitive, multi-AGC kinase inhibitor with IC₅₀s 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.

SB-772077B dihydrochloride is an orally active aminofuran-based Rho kinase ((ROCK)) inhibitor with IC₅₀ values of 5.6 nM and 6 nM for ROCK1 and ROCK2, respectively. SB-772077B dihydrochloride reduces inflammatory cytokines (TNF-α and IL-6). SB-772077B dihydrochloride relaxes aortic rings and lowers blood pressure. SB-772077B dihydrochloride can be used in the research of inflammatory diseases.