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ROCK

Rocks are serine/threonine kinases which are involved in cell motility, cell proliferation and apoptosis. The activity of ROCK can be regulated in different ways in different condition. During apoptosis, caspase-3 cleaves the carboxy-terminal region of ROCKs to free the activity of ROCKs. The kinase activity of ROCKs is moderately enhanced after Rho binding. Small GTP-binding proteins, Gem and Rad, function as negative regulators of ROCKs.  ROCKs can phosphorylate LIM kinase, myosin light chain (MLC) and MLC phosphatase to increase actin-filament assembly and actomyosin contraction. In response to sphingosine-1-phosphate (S1P) binding to G-protein-coupled receptors (GPCR), Rho can be activated by guanine nucleotide exchange factors (GEFs) that are themselves activated. ROCK can also influence the insulin signaling pathway to interface cell.

Inhibitors

Cat.No. Product Name Information Publication Customer Review
S1049 Y-27632 2HCl Y-27632 2HCl is a selective ROCK1 (p160ROCK) inhibitor with Ki of 140 nM. (1)
S1459 Thiazovivin Thiazovivin (Tzv) is a novel ROCK inhibitor with IC50 of ~0.5 μM. (1)
S1474 GSK429286A GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.

ROCK

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