ROCK Inhibitor

ROCK2-IN-11 (Compound A20) is a selective ROCK2 inhibitor with an IC₅₀ of 0.18 μM for ROCK2 over ROCK1. ROCK2-IN-11 can be used for idiopathic pulmonary fibrosis and cGVHD research.

ROCK-IN-5 (compound I-B-37) is a potent inhibitor of ROCK, ERK, GSK, and AGC protein kinases. ROCK-IN-5 has the potential for proliferative, cardiac and neurodegenerative diseases research.

Rhodblock 1a is an inhibitor of the Rho kinase signaling pathway. It inhibits the normal formation of the cleavage furrow during cell division by interfering with the localization and function of Rho pathway proteins, causing some cells to fail to form a cleavage furrow or the formed cleavage furrow to break, resulting in binucleated cells. Rhodblock 1a can be used to study the mechanism of cell division and is expected to be used in the research of diseases such as cardiovascular diseases and cancer.

ROCK/HDAC-IN-1 (Compound 10h) is an orally active ROCK/HDAC inhibitor. ROCK/HDAC-IN-1 inhibits ROCK1/2 (IC₅₀: 254.9 nM, 58.18 nM) and HDAC1/2/3/6/8 (IC₅₀: 9.09, 8.03, 6.26, 0.41, 7.69 nM). ROCK/HDAC-IN-1 stimulates the activation of DAMPs, specifically Calreticulin (CRT) exposure and HMGB1 release, indicating that it is a potential ICD inducer.. ROCK/HDAC-IN-1 has antiproliferative activity against breast cancer cells (IC₅₀: 0.37 μM for MDA-MB-231 cell), and inhibits tumor growth and activates T cells without apparent toxicity.

Verosudil (AR-12286) hydrochloride is the hydrochloride form of Verosudil (HY-16758). Verosudil hydrochloride is a ROCK inhibitor. Verosudil hydrochloride has equal inhibitory activity against ROCK1 and ROCK2 (K_i: 2 nM). Verosudil hydrochloride is less selective for PKA, PKCT, MRCKA, and CAM2A (K_i: 69 nM, 9322 nM, 28 nM, 5855 nM, respectively). Verosudil hydrochloride increases trabecular outflow capacity to reduce intraocular pressure. Verosudil hydrochloride is useful in the study of glaucoma and ocular hypertension.

BIPM is a potent ROCK2 inhibitor. BIPM leads to significant changes in neurite length, cell migration and actin stress fibers. BIPM plays an important role in anti-cancer metastasis.

Khasianine (Standard) is the analytical standard of Khasianine (HY-N2322). This product is intended for research and analytical applications. Khasianine is a steroidal glycoalkaloid. Khasianine alleviates psoriasis-like skin inflammation by inhibiting the TNF-α/NF-κB axis. Khasianine can downregulate the RhoA pathway and exhibits potential antimetastatic activity. Khasianine upregulates the expression of TNFR I and TNFR II without inducing apoptotic effects. Khasianine can be used in studies related to psoriasis, pancreatic ductal adenocarcinoma, and liver cancer.

ROCK2-IN-9 (compound 7u) is a selective ROCK2 inhibitor (IC₅₀=36.8 nM) with anticancer activity. ROCK2-IN-9 inhibits cancer cell migration and invasion by regulating multiple cellular activities of the actin cytoskeleton. ROCK2-IN-9 can be used in breast cancer research.

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.

Fimosudil (ROCK2-IN-6) (Comp A) is a selective ROCK2 inhibitor, can be used for ROCK mediated diseases, autoimmune diseases and inflammation research.

Y-33075 hydrochloride (Y-39983) is a selective ROCK inhibitor derived from Y-27632, and is more potent than Y-27632, with an IC₅₀ of 3.6 nM.

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.

RX-021 is a ROCK1 and ROCK2 inhibitor with IC₅₀ values of 30.01 nM and 34.31 nM, respectively. RX-021 induces reversible morphological changes in human trabecular meshwork cells, maintains the survival of retinal ganglion cells, restores electroretinogram responses, and improves retinal histopathological changes. RX-021 achieves sustained reduction of intraocular pressure in a mouse model of ocular hypertension. RX-021 can be used for the research of glaucoma.

ROCK-IN-32 is a ROCK inhibitor, with an IC₅₀ value of 11 nM for ROCK2. ROCK-IN-32 can be used in research of cardiovascular disease, cancer and inflammation.

GSK317354A is a ROCK and GRK inhibitor. GSK317354A can be used for heart failure and Parkinson’s disease research.

ROCK-IN-7 (compound 9) is a ROCK kinase inhibitor. ROCK-IN-7 can be used for research in ocular diseases (such as glaucoma and retinal diseases).

4-(Indolin-1-yl) pyrimidin-2-amine (13a, non-salt form) is a ROCK inhibitor.

ROCK-IN-8 (Example 4) is a ROCK inhibitor, with an IC₅₀ value less than 100 nM. ROCK-IN-8 has anti-inflammatory activity. ROCK-IN-8 can be used for research of respiratory and gastro-intestinal diseases.

GSK2163632A is a selective G protein-coupled receptor kinase (GRK) inhibitor that can be used as a probe for studying heart failure and Parkinson's disease. GSK2163632A potently inhibits GRK1 and GRK5, and also inhibits Rho-associated coiled-coil kinase (ROCK) and insulin-like growth factor receptor IGF-1R. GSK2163632A binds to GRK2 in a manner similar to Paroxetine (HY-122272).

KD025m1 is a novel selective ROCK2 inhibitor. KD025m1 has good anti obesity, improved insulin sensitivity, and blood glucose control effects. KD025m1 can be used to study metabolic diseases such as diabetes and obesity.