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2095432-71-4

2095432-71-4 structure
2095432-71-4 structure
  • Name: GSK269962 HCl
  • Chemical Name: GSK269962A hydrochloride
  • CAS Number: 2095432-71-4
  • Molecular Formula: C29H31ClN8O5
  • Molecular Weight: 607.06
  • Catalog: Signaling Pathways Cell Cycle/DNA Damage ROCK
  • Create Date: 2020-06-01 21:46:21
  • Modify Date: 2024-01-22 20:45:53
  • 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].

Name GSK269962A hydrochloride
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
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.

Molecular Formula C29H31ClN8O5
Molecular Weight 607.06