1. Cell Cycle/DNA Damage
    Stem Cell/Wnt
    Cytoskeleton
    TGF-beta/Smad
  2. ROCK
  3. GSK269962A

GSK269962A (Synonyms: GSK 269962)

Cat. No.: HY-15556 Purity: 98.12%
Handling Instructions

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

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

GSK269962A Chemical Structure

GSK269962A Chemical Structure

CAS No. : 850664-21-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 121 In-stock
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 720 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

GSK269962A (GSK 269962) is a potent ROCK inhibitor with IC50s of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively. GSK269962A 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

570.60

Formula

C₂₉H₃₀N₈O₅

CAS No.

850664-21-0

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (52.58 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7525 mL 8.7627 mL 17.5254 mL
5 mM 0.3505 mL 1.7525 mL 3.5051 mL
10 mM 0.1753 mL 0.8763 mL 1.7525 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.62 mg/mL (1.09 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 0.62 mg/mL (1.09 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 0.62 mg/mL (1.09 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 98.12%

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Keywords:

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

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GSK269962A
Cat. No.:
HY-15556
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