assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Quality Level
Biochem/physiol Actions
Orally available, potent and selective ROCK1/2 inhibitor that impacting vasodilation and AML cell viability; selective probe for Rho-kinase signaling pathways.
GSK269962A (GSK269962) is a potent (ROCK1 IC50 1.6 nM; ROCK2 IC50 4-6 nM), selective, orally bioavailable inhibitor of ROCK kinases. Offering greater selectivity than Y-27632 and Fasudil, it weakly inhibits MSK1 (IC50 49 nM) and RSK1 (IC50 132 nM). As an ATP-competitive inhibitor, it blocks ROCK-mediated phosphorylation of downstream targets (e.g., MLC, MYPT1), causing significant functional outcomes including smooth muscle relaxation (vasorelaxation IC50 35 nM), actin stress fiber disruption, G2 cell cycle arrest, and apoptosis, notably in AML models (proliferation IC50 0.61-1337 nM). In vitro, it inhibits AngII-induced stress fibers and inflammatory cytokine production. With demonstrated in vivo efficacy lowering blood pressure in hypertensive rats and reducing leukemia burden in AML xenografts, GSK269962A serves as a valuable tool for studying ROCK signaling in cytoskeleton regulation, smooth muscle contraction, cell migration, proliferation, and survival.
GSK269962A (GSK269962) is a potent (ROCK1 IC50 1.6 nM; ROCK2 IC50 4-6 nM), selective, orally bioavailable inhibitor of ROCK kinases. Offering greater selectivity than Y-27632 and Fasudil, it weakly inhibits MSK1 (IC50 49 nM) and RSK1 (IC50 132 nM). As an ATP-competitive inhibitor, it blocks ROCK-mediated phosphorylation of downstream targets (e.g., MLC, MYPT1), causing significant functional outcomes including smooth muscle relaxation (vasorelaxation IC50 35 nM), actin stress fiber disruption, G2 cell cycle arrest, and apoptosis, notably in AML models (proliferation IC50 0.61-1337 nM). In vitro, it inhibits AngII-induced stress fibers and inflammatory cytokine production. With demonstrated in vivo efficacy lowering blood pressure in hypertensive rats and reducing leukemia burden in AML xenografts, GSK269962A serves as a valuable tool for studying ROCK signaling in cytoskeleton regulation, smooth muscle contraction, cell migration, proliferation, and survival.
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Ting Pan et al.
Frontiers in pharmacology, 13, 1064470-1064470 (2022-12-24)
Acute myeloid leukemia (AML) is an aggressive hematologic malignancy with high mortality that urgently requires new treatments. ROCK1 plays an essential role in regulating growth and survival in AML cells. In this study, we evaluated GSK269962A, a selective ROCK1 inhibitor
Chris Doe et al.
The Journal of pharmacology and experimental therapeutics, 320(1), 89-98 (2006-10-05)
Increased Rho kinase (ROCK) activity contributes to smooth muscle contraction and regulates blood pressure homeostasis. We hypothesized that potent and selective ROCK inhibitors with novel structural motifs would help elucidate the functional role of ROCK and further explore the therapeutic
Andrzej Wróbel et al.
European journal of pharmacology, 837, 127-136 (2018-09-03)
Literature data give clear evidence that upregulated RhoA/Rho-kinase signalling is one of the factors that may lead to the development of detrusor overactivity and various disorders of the central nervous system. Therefore, the main objective of our study was to
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