ROCK

ROCK

The AGC (PKA/PKG/PKC) family of serine-threonine kinases includes ROCK (Rho-associated protein kinase). Animals such as chicken, zebrafish, Xenopus, and mammals also have ROCKs (ROCK1 and ROCK2). With a molecular weight of 158 kDa, human ROCK1 is a significant RhoA small GTPase downstream effector. A kinase domain, an acoiled-coil region, and a Pleckstrin homology (PH) domain make up a mammalian ROCK. If RhoA-GTP is absent, the kinase activity of ROCKs is reduced by an autoinhibitory intramolecular fold. Since ROCK is a downstream effector protein of the small GTPase Rho, one of the primary regulators of the cytoskeleton, ROCK is involved in a variety of different cellular phenomena.

ROCK related products

Structure Cat No. Product Name CAS No. Product Description
V1346 RKI-1447 1342278-01-6 RKI-1447 (ROCK Inhibitor XIII; RKI 1447; RKI1447) is a potent small molecule inhibitor of ROCK1 and ROCK2 with potential antitumor activities againstbreast cancer.
V55726 ROCK-IN-5 692870-25-0 ROCK-IN-5 (compound IB-37) is a potent inhibitor of ROCK, ERK, GSK and AGC protein kinases.
V55727 ROCK-IN-6 2489328-74-5 ROCK-IN-6 is a potent ROCK2 inhibitor (antagonist) with IC50 of 2.19 nM.
V55725 ROCK-IN-7 2376635-95-7 ROCK-IN-7 (compound 9) is a ROCK kinase inhibitor.
V55724 ROCK-IN-8 1621103-79-4 ROCK-IN-8 (Example 4) is a ROCK inhibitor (antagonist) with IC50 of less than 100 nM.
V55728 ROCK-IN-9 2643334-76-1 ROCK-IN-9 (Compound T345) is a ROCK inhibitor.
V55729 ROCK2-IN-6 2260506-59-8 ROCK2-IN-6 (Comp A) is a selective ROCK2 inhibitor for the study of ROCK-mediated diseases, autoimmune diseases, and inflammation.
V53327 ROCK2-IN-6 hydrochloride 2762238-94-6 ROCK2-IN-6 HCl (Comp A) is a selective ROCK2 inhibitor for research into ROCK-mediated diseases, autoimmune diseases, and inflammation.
V2556 SAR-020106 1184843-57-9 SAR-020106 is a potent,ATP-competitive, and selective CHK1 inhibitor with an IC50 of 13.3 nM on isolated human enzyme.
V3093 SAR-407899 923359-38-0 SAR407899 is a novel, potent, selective, and ATP-competitiveROCKinhibitor with anIC50of 135 nM forROCK-2, andKis of 36 nM and 41 nM for human and ratROCK-2, respectively.
V35267 Sovesudil (PHP-201; AMA0076) 1333400-14-8 Sovesudil (PHP-201) is a potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor (antagonist) with IC50s of 3.7 and 2.3 nM for ROCK I and ROCK II, respectively.
V1343 Thiazovivin 1226056-71-8 Thiazovivin (TZV) is a novel, selective, and cell-permeable small molecule ROCK (Rho-associated kinase) inhibitor with an IC50 of 0.5 μM in a cell-free assay.
V35201 THK01 2226941-26-8 THK01 is a potent ROCK2 inhibitor (antagonist) with IC50s of 5.7 and 923 nM for ROCK2 and ROCK1, respectively.
V2557 THZ1 1604810-83-4 THZ1 (THZ-1) is a novel, potent, selective and covalent/irreversible CDK7 inhibitor (IC50 = 3.2 nM) with anticancer activity.
V1184 Wogonin 632-85-9 Wogonin (Vogonin), a naturally occurring and pharmacologically-active flavonoid found in plants, has been reported to exhibit anticancer effects against various cancer cell types such as osteosarcoma, leukemia, breast cancer and glioma.
V3416 Y-27632 146986-50-7 Y-27632 is a potent and selective inhibitor of ROCK1 (p160ROCK) with IC50 of 140 nM in a cell-free assay, it exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK.
V1342 Y-27632 2HCl 129830-38-2 Y-27632 2HCl (Y27632;Y2 7632), the dihydrochloride salt ofY-27632,is a novel, potent and selective inhibitor of ROCK1 (p160ROCK) with potential antifibrotic and anticancer activity.
V26655 Y-33075 hydrochloride (Y-39983) 471843-75-1 Y-33075 HCl (Y-39983) is a selective ROCK inhibitor, derived from Y-27632, with IC50 of 3.6 nM, which is more effective than Y-27632.
V3415 Y-39983 199433-58-4 Y-39983 (also calledY-33075)is a novel, potent and selective inhibitor of Rho-associated coiled coil-forming protein kinase( ROCK ) with IC50 values of 3.6 nM, 0.42 μM and 0.81 μM for ROCK, PKC and CaMKII, respectively.
V2559 Y-39983 HCl (Y-33075) 173897-44-4 Y-39983 HCl (also calledY-33075)is a novel, potent and selective inhibitor of Rho-associated coiled coil-forming protein kinase( ROCK ) with IC50 values of 3.6 nM, 0.42 μM and 0.81 μM for ROCK, PKC and CaMKII, respectively.
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