GSK269962A Chemical Properties

Melting point:

125 - 127°C

Density 

1.45

storage temp. 

under inert gas (nitrogen or Argon) at 2–8 °C

solubility 

DMSO (Slightly), Methanol (Slightly)

form 

Solid

pka

13.19±0.70(Predicted)

color 

Off-White

GSK269962A Usage And Synthesis

Description

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.

Uses

GSK 269962 is a potent and selective Rho kinase (ROCK) inhibitor.

storage

Store at +4°C