ROCK Inhibitor

(Rac)-NRL-1049 is the racemic mixture of NRL-1049 (BA-1049 (free base)) (HY-162596). NRL-1049 is an orally available and selective ROCK2 inhibitor with IC₅₀ values of 0.59 µM for ROCK2 and 26 µM for ROCK1, respectively. NRL-1049 modulates ROCK signaling, preserves blood-brain barrier integrity, reduces edema, seizures and hemorrhage, and alleviates cerebral cavernous malformation lesion burden. NRL-1049 can be used for the study of acute brain injury, ischemic stroke, and cerebral cavernous malformations.

Bazipsudil is a potent, selective Rho-associated protein kinase (ROCK) inhibitor.

CCG-232964 is an orally active inhibitor of Rho/MRTF/SRF. CCG-232964 inhibits LPA-induced CTGF gene expression.

WF-536 is an orally active inhibitor of Rho-associated coiled-coil-containing protein kinase (ROCK). WF-536 has tumor anti-metastatic activity. WF-536 can be used for the research of cancer.

ROCK-IN-11 (example 94) is a potent inhibitor of ROCK1 and ROCK2, with the IC₅₀ of ≤ 5μM. ROCK-IN-11 plays an important role in cancer research.

ROCK-IN-12 (compound R3) is a selective ROCK inhibitor. ROCK-IN-12 can be used in the study of glaucoma.

3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine (Compound 7) is an inhibitor of protein kinases, with IC₅₀s of 0.092, 0.26, 0.77 μM for PKC-α, ROCK, ASK1. 3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine shows potent cytotoxicity against PC-3 cancer cells with an IC₅₀ value of 0.16 μM.

ROCK-IN-D2 is a potent and selective ROCK inhibitor.

ROCK-IN-4 is a potent ROCK inhibitor maintaining NO releasing ability. ROCK-IN-4 reversibly depolymerizes F-actin, and suppresses mitochondrial respiration in human trabecular meshwork (HTM) cells. ROCK-IN-4 can be used for glaucoma or ocular hypertension research.

OXA-06 is a pharmacologic inhibitor of ROCK, possessing antitumor activity by impairing cell migration and MYPT1 phosphorylation in PANC-1 cells.

GKI-1 (Standard) is the analytical standard of GKI-1 (HY-100521). This product is intended for research and analytical applications. GKI-1 is a Greatwall (GWL) kinase inhibitor with IC50s of 4.9 and 2.5 μM against hGWLFL and hGWL-KinDom, respectively. GKI-1 robustly inhibits ROCK1 with an IC50 of 11 μM, but only weakly affected PKA.

Cotosudil hydrochloride is a ROCK kinase inhibitor that can be used in studies on glaucoma or ocular hypertension.

AS1892802 (Standard) is the analytical standard of AS1892802 (HY-108519). This product is intended for research and analytical applications. AS1892802 is a potent, orally active, and highly selective inhibitor of ROCK. The onset of antinociceptive effect of AS1892802 is as fast as those of Tramadol and Diclofenac. AS1892802 did not induce gastric irritation or abnormal behavior. AS1892802 is an attractive analgesic profile for the research of severe osteoarthritis pain.

Rho-Kinase-IN-1 (Standard) is the analytical standard of Rho-Kinase-IN-1 (HY-100270). This product is intended for research and analytical applications. 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.

Cinnamyl Alcohol-d₅ is deuterated labeled Cinnamyl Alcohole (HY-Y0045). Cinnamyl Alcohol is an active component from chestnut flower, inhibits increased PPARγ expression, exhibits anti-obesity, antioxidant and anti-inflammatory activities.

Thiazovivin (Standard) is the analytical standard of Thiazovivin (HY-13257). This product is intended for research and analytical applications. Thiazovivin is a potent ROCK inhibitor, which can protect human embryonic stem cells. Thiazovivin improves the efficiency of iPSC generation.

ROCK2-IN-2 (Standard) is the analytical standard of ROCK2-IN-2 (HY-103620). This product is intended for research and analytical applications. ROCK2-IN-2 is a selective ROCK2 inhibitor extracted from patent US20180093978A1, Compound A-30, has an IC₅₀ of <1 μM.

RK_i-1447 dihydrochloride (Standard) is the analytical standard of RK_i-1447 (dihydrochloride) (HY-110339). This product is intended for research and analytical applications. RK_i 1447 dihydrochloride is a potent and selective ROCK inhibitor with IC₅₀s of 14.5 and 6.2 nM for ROCK1 and ROCK2, respectively. RK_i 1447 dihydrochloride suppresses colorectal carcinoma cell growth and promotes apoptosis.

CMPD101 (Standard) is the analytical standard of CMPD101 (HY-103045). This product is intended for research and analytical applications. 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.

SB-772077B dihydrochloride (Standard) is the analytical standard of SB-772077B (dihydrochloride) (HY-108518). This product is intended for research and analytical applications. SB-772077B dihydrochloride is an orally active aminofuran-based Rho K_inase ((ROCK)) inhibitor with IC₅₀ values of 5.6 nM and 6 nM for ROCK1 and ROCK2, respectively. SB-772077B dihydrochloride reduces inflammatory cytoK_ines (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.