GSK269962

Two Rho-associated kinases (ROCKS), ROCK1 and ROCK2, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. GSK269962 is a selective ROCK inhibitor with IC50 values of 1.6 and 6 nM for ROCK1 and ROCK2, respectively. It displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases. GSK269962 has been shown to block the generation of inflammatory cytokines in lipopolysaccharide-stimulated monocytes and to induce vasorelaxation in preconstricted rat aorta (IC50 = 35 nM). Oral administration of 1-30 mg/kg GSK269962 can dose-dependently lower blood pressure in spontaneously hypertensive rats.Formal Name: N-[3-[[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-6-yl]oxy]phenyl]-4-[2-(4-morpholinyl)ethoxy]-benzamide. CAS Number: 850664-21-0. Synonyms: GSK269962A, GSK269962B. Molecular Formula: C29H30N8O5. Formula Weight: 570.6. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 16 mg/ml, DMF:PBS(pH7.2) (1:2): 0.3 mg/ml, DMSO: 14 mg/ml. lambdamax: 275 nm. SMILES: O=C(NC1=CC=CC(OC2=NC=C(N=C(C3=NON=C3N)N4CC)C4=C2)=C1)C(C=C5)=CC=C5OCCN6CCOCC6. InChi Code: InChI=1S/C29H30N8O5/c1-2-37-24-17-25(31-18-23(24)33-28(37)26-27(30)35-42-34-26)41-22-5-3-4-20(16-22)32-29(38)19-6-8-21(9-7-19)40-15-12-36-10-13-39-14-11-36/h3-9,16-18H,2,10-15H2,1H3,(H2,30,35)(H,32,38). InChi Key: YOVNFNXUCOWYSG-UHFFFAOYSA-N.