ROCK
Rho-associated protein kinase; Rho-associated kinase; Rho-kinase; ROK
ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC (PKA/ PKG/PKC) family of serine-threonine kinases. ROCKs (ROCK1 and ROCK2) occur in mammals, zebrafish, Xenopus, invertebrates and chicken. Human ROCK1 has a molecular mass of 158 kDa and is a major downstream effector of the small GTPase RhoA. Mammalian ROCK consists of a kinase domain, acoiled-coil region and a Pleckstrin homology (PH) domain, which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular fold if RhoA-GTP is not present. ROCK plays a role in a wide range of different cellular phenomena, as ROCK is a downstream effector protein of the small GTPase Rho, which is one of the major regulators of the cytoskeleton.
ROCK Isoform Specific Products
All Product Categories
-
ROCK Related Products (198)
Related Products (198)
-
Antibodies (12)
-
ROCK Isoform Comparison
-
Fasudil hydrochloride semihydrate
0 ImagesCat. No.: HY-10341BCAS No.: 186694-02-0Synonyms: HA-1077 hydrochloride semihydrate; AT877 hydrochloride semihydrateFasudil (HA-1077; AT877) hydrochloride semihydrate is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki 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 semihydrate is also a potent Ca2+ channel antagonist and vasodilator.
-
Rhodblock 1a
0 ImagesCat. No.: HY-134913CAS No.: 701226-08-6Rhodblock 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
0 ImagesCat. No.: HY-168650ROCK/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 hydrochloride
0 ImagesCat. No.: HY-16758ACAS No.: 1414854-44-6Synonyms: AR-12286 hydrochlorideVerosudil (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 (Ki: 2 nM). Verosudil hydrochloride is less selective for PKA, PKCT, MRCKA, and CAM2A (Ki: 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
0 ImagesCat. No.: HY-100460CAS No.: 1070424-33-7BIPM 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.
-
ROCK2-IN-9
0 ImagesCat. No.: HY-162798ROCK2-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.
-
Fimosudil
0 ImagesCat. No.: HY-156592CAS No.: 2260506-59-8Synonyms: ROCK2-IN-6Fimosudil (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
0 ImagesCat. No.: HY-10068CAS No.: 471843-75-1Synonyms: Y-39983Y-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.
-
RX-021
0 ImagesCat. No.: HY-187203RX-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
0 ImagesCat. No.: HY-113641CAS No.: 1013117-40-2ROCK-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
0 ImagesCat. No.: HY-111239CAS No.: 874119-13-8GSK317354A is a ROCK and GRK inhibitor. GSK317354A can be used for heart failure and Parkinson’s disease research.
-
ROCK-IN-7
0 ImagesCat. No.: HY-153569CAS No.: 2376635-95-7ROCK-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
0 ImagesCat. No.: HY-W1058961CAS No.: 1401661-20-84-(Indolin-1-yl) pyrimidin-2-amine (13a, non-salt form) is a ROCK inhibitor.
-
ROCK-IN-8
0 ImagesCat. No.: HY-156550CAS No.: 1621103-79-4ROCK-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
0 ImagesCat. No.: HY-118046CAS No.: 1123163-20-1GSK2163632A 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).
-
Desisopropyle-belumosudil
0 ImagesCat. No.: HY-164809CAS No.: 911417-89-5
-
Chloroxoquinoline
0 ImagesCat. No.: HY-W110138CAS No.: 23833-97-8Chloroxoquinoline is an anticancer agent. Chloroxoquinoline damages the DNA templates of cancer cells, inducing DNA breaks and cell death, and inhibits cell invasion via down-regulating Rho/Rho kinase signaling pathway. Chloroxoquinoline enhances the radiation sensitivity of Lewis lung cancer cells and xenograft tumors in tumor-bearing mouse models but decreases efficacy after long term exposure in rat models by auto-induction effects on CYP1A and CYP3A. Chloroxoquinoline has a broad-spectrum anticancer activity, such as non-small-cell lung carcinoma (NSCLC), breast cancer and gastric cancer.
