GSK269962 HCl

Names

[ CAS No. ]:
2095432-71-4

[ Name ]:
GSK269962 HCl

Biological Activity

[Description]:

GSK269962A hydrochloride (GSK 269962 hydrochloride) is a potent ROCK inhibitor with IC50s of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively. GSK269962A hydrochloride has anti-inflammatory and vasodilatory activities[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Cell Cycle/DNA Damage >> ROCK

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Stem Cell/Wnt >> ROCK

Signaling Pathways >> TGF-beta/Smad >> ROCK

[Target]

ROCK1:1.6 nM (IC50)

ROCK2:4 nM (IC50)

RSK1:132 nM (IC50)

MSK1:49 nM (IC50)

AKT1:955 nM (IC50)

AKT2:1350 nM (IC50)

AKT3:1510 nM (IC50)

CDK2:3500 nM (IC50)

GSK3α:1260 nM (IC50)

[In Vitro]

GSK269962A has an IC50 of 1.6 nM toward recombinant human ROCK1. GSK269962A exhibits more than 30-fold selectivity against a panel of serine/threonine kinases[1]. GSK269962A induces vasorelaxation in preconstricted rat aorta with an IC50 of 35 nM[1].

[In Vivo]

GSK269962A is a potent antihypertensive agent. GSK269962A (0.3, 1, and 3 mg/kg; oral gavage) induces a dose-dependent reduction in blood pressure in spontaneously hypertensive rat (SHR). The reduction of blood pressure is acute and substantial[1]. Animal Model: Male Sprague-Dawley rats (350-400g)[1] Dosage: 0.3, 1, and 3 mg/kg Administration: Oral gavage; 12 hours Result: Induced a dose-dependent reduction in blood pressure.

[References]

[1]. Doe C, et al. Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. J Pharmacol Exp Ther. 2007 Jan;320(1):89-98.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₉H₃₁ClN₈O₅

[ Molecular Weight ]:
607.06

GSK269962 HCl

Names

Biological Activity

Chemical & Physical Properties

Related Compounds