A selective ROCK inhibitor (IC50s = 1.6 and 6 nM for ROCK-I and ROCK-II

GSK269962 – 5 mg

Brand:
Cayman
CAS:
850664-21-0
Storage:
-20
UN-No:
Non-Hazardous - /

Two Rho-associated kinases (ROCKS), ROCK-I and ROCK-II, 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 ROCK-I and ROCK-II, respectively.{16599} It displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases.{16599} 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).{16599} Oral administration of 1-30 mg/kg GSK269962 can dose-dependently lower blood pressure in spontaneously hypertensive rats.{16599}  

 

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Description

A selective ROCK inhibitor (IC50s = 1.6 and 6 nM for ROCK-I and ROCK-II, respectively); blocks the generation of inflammatory cytokines in LPS-stimulated monocytes and induces vasorelaxation in preconstricted rat aorta (IC50 = 35 nM)

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

Synonyms:  GSK269962A|GSK269962B

Molecular weight: 570.6

CAS: 850664-21-0

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|ROCK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Vasculature|Vasodilation||Research Area|Immunology & Inflammation|Innate Immunity

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