ROCK Inhibitor

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.

Belumosudil (mesylate) (Standard) is the analytical standard of Belumosudil (mesylate). This product is intended for research and analytical applications. 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.

Hydroxyfasudil (hydrochloride) (Standard) is the analytical standard of Hydroxyfasudil (hydrochloride). This product is intended for research and analytical applications. Hydroxyfasudil hydrochloride is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.

GSK429286A (Standard) is the analytical standard of GSK429286A (HY-11000). This product is intended for research and analytical applications. GSK429286A is a selective inhibitor of ROCK1 with an IC₅₀ value of 14 nM.

Y-30141 is a hinge-binding 7-azaindole-based Rho kinase (ROCK) inhibitor. Y-30141 can be used for the research of hypertension.

HA-100 (Standard) is the analytical standard of HA-100 (HY-100984). This product is intended for research and analytical applications. HA-100 is a potent protein kinase inhibitor, with IC50s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. HA-100 also used as a ROCK inhibitor.

BAY-549 (Standard) is the analytical standard of BAY-549 (HY-10319). This product is intended for research and analytical applications. 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.

Hydroxyfasudil (Standard) is the analytical standard of Hydroxyfasudil. This product is intended for research and analytical applications. Hydroxyfasudil is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.

Belumosudil (Standard) is the analytical standard of Belumosudil. This product is intended for research and analytical applications. Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties.

ROCK-IN-18 is a blood-brain barrier-permeable selective inhibitor of the ROCK2 protein kinase. ROCK-IN-18 is applicable to research related to cardiovascular diseases, neurological diseases, breast cancer, colon cancer, pancreatic cancer and other disorders.

Y-27632 (Standard) is the analytical standard of Y-27632 (HY-10071). This product is intended for research and analytical applications. 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.

Belumosudil-d₇ (KD025-d₇) is deuterium labeled Belumosudil. Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC₅₀s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties.

ROCK-IN-13 is a ROCK2 inhibitor with an IC₅₀ of 8 nM against human ROCK2. ROCK-IN-13 has the potential for use in the research of diseases such as multiple sclerosis, glaucoma, and cardiovascular diseases.

Cinnamyl Alcohol-d₉ 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.

Cinnamyl Alcohol (Standard) is the analytical standard of Cinnamyl Alcohole (HY-Y0078). This product is intended for research and analytical applications. Cinnamyl Alcohol is an active component from chestnut flower, inhibits increased PPARγ expression, exhibits anti-obesity, antioxidant and anti-inflammatory activities.

Sovesudil hydrochloride (Standard) is the analytical standard of Sovesudil (hydrochloride) (HY-109191A). This product is intended for research and analytical applications. Sovesudil (PHP-201) hydrochloride is a potent, ATP-competitive, locally acting Rho K_inase (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.

Nocarnickelamide B (Compound 2) is a linear peptide and ROCK1/2 inhibitor. Nocarnickelamide B exhibits dual inhibitory activity against ROCK1 and ROCK2 with IC₅₀s of 14.9 μM and 21.9 μM, respectively. Nocarnickelamide B binds to the ATP-binding site. Nocarnickelamide B inhibits the activation of ROCK-regulated cytoskeletal contraction markers such as the myosin light chain. Nocarnickelamide B is potential for glaucoma reasearch.