ROCK Inhibitor

Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and CNS-penetrant Rho Kinase (ROCK) inhibitor (ROCK2 IC₅₀ = 3 nM). Rho-Kinase-IN-2 can be used in Huntington’s research.

THK01 is a potent ROCK2 inhibitor with IC₅₀ values of 5.7 and 923 nM for ROCK2 and ROCK1, respectively. THK01 inhibits breast cancer metastasis through the ROCK2-STAT3 signaling pathway. THK01 can be used in research of breast cancer.

GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC₅₀=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC₅₀=398 nM, p70S6K: IC₅₀=1 μM). GSK-25 inhibits P450 profile (IC₅₀s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively).

ROCK2-IN-8 (Compound 1) is an orally active ROCK2 inhibitor, with an IC₅₀ of 7.2 nM. ROCK2-IN-8 can be used for the research of aqueous humor outflow in porcine eyes and myosin light chain phosphorylation.

RKI 1447 dihydrochloride is a potent and selective ROCK inhibitor with IC₅₀s of 14.5 and 6.2 nM for ROCK1 and ROCK2, respectively. RKI 1447 dihydrochloride suppresses colorectal carcinoma cell growth and promotes apoptosis.

Sovesudil (PHP-201) hydrochloride is a potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor with IC₅₀s of 3.7 and 2.3 nM for ROCK-I and ROCK-II, respectively. Sovesudil hydrochloride lowers intraocular pressure (IOP) without inducing hyperemia.

ROCK1-IN-1 is a potent selective ROCK1 inhibitor with a K_i of 540 nM. ROCK1-IN-1 can be used for the research of hypertension.

CRT0066854 hydrochloride is a potent and selective atypical PKCs 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.

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

RhoA-ROCK-IN-1 (Compound b19) is an inhibitor of RhoA/ROCK. RhoA-ROCK-IN-1 can significantly inhibit cell proliferation, migration, and invasion, while promoting cell apoptosis. RhoA-ROCK-IN-1 demonstrates remarkable anticancer activity by inhibiting the RhoA/ROCK pathway.

Cotosudil is a ROCK kinase inhibitor, which can be used for glaucoma or ocular hypertension research.

ROCK2 Human Pre-designed siRNA Set A contains three designed siRNAs for ROCK2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Scaff10-8 is a RhoA inhibitor. Scaff10-8 binds to RhoA, inhibits AKAP-Lbc-mediated RhoA activation. Scaff10-8 can be used for research on diabetes insipidus and bipolar disorder.

LIMK-IN-1 (Compound 14) is an inhibitor of LIM-Kinase (LIMK), with IC₅₀s of 0.5 nM and 0.9 nM for LIMK1 and LIMK2, respectively. LIMK-IN-1 can be used for ocular hypertension and associated glaucoma research.

HSD1590 is potent ROCK inhibitor, with IC₅₀s of 1.22 and 0.51 nM for ROCK1 and ROCK2, respectively. HSD1590 exhibits single digit nanomolar binding to ROCK (K_ds<2 nM). HSD1590 displays low cytotoxicity.

OXA-06 hydrochloride is an ATP-competitive ROCK inhibitor that blocks anchorage-dependent growth and invasion of non-small cell lung cancer cell lines. OXA-06 hydrochloride inhibits cofilin phosphorylation but does not stimulate apoptosis.

ROCK1 Human Pre-designed siRNA Set A contains three designed siRNAs for ROCK1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

NRL-1049 dihydrochloride (BA-1049) is a selective and orally active rho-associated protein kinase 2 (ROCK2) inhibitor with an IC₅₀ of 0.59 μM. NRL-1049 dihydrochloride shows selectivity for ROCK2 is 44 times that of ROCK1 (IC₅₀ = 26 μM). NRL-1049 dihydrochloride can preserve the blood-brain barrier after acute injury.

Glycyl H-1152 hydrochloride (compound 18) is a glycyl derivative of Rho-kinase inhibitors H-1152 dihydrochloride. Glycyl H-1152 hydrochloride inhibits ROCKII, Aurora A, CAMKII and PKG, with IC₅₀s of 0.0118, 2.35, 2.57 and 3.26 μM respectively. Glycyl H-1152 hydrochloride has higher selective than H-1152 hydrochloride.

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