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  2. ROCK
  3. GSK269962A hydrochloride

GSK269962A hydrochloride (Synonyms: GSK 269962 hydrochloride)

Cat. No.: HY-15556A
Handling Instructions

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.

For research use only. We do not sell to patients.

GSK269962A hydrochloride Chemical Structure

GSK269962A hydrochloride Chemical Structure

CAS No. : 2095432-71-4

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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].

IC50 & Target[1]

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.
Molecular Weight

607.06

Formula

C₂₉H₃₁ClN₈O₅

CAS No.

2095432-71-4

SMILES

CCN1C2=CC(OC3=CC=CC(NC(C4=CC=C(OCCN5CCOCC5)C=C4)=O)=C3)=NC=C2N=C1C6=NON=C6N.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

GSK269962AGSK 269962GSK269962GSK-269962ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKROCK1ROCK2anti-inflammatoryvasodilatorycardiovascularantihypertensivebloodpressureInhibitorinhibitorinhibit

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GSK269962A hydrochloride
Cat. No.:
HY-15556A
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