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

GSK429286A 

Cat. No.: HY-11000 Purity: 99.13%
Handling Instructions

GSK429286A is a selective inhibitor of ROCK1 with an IC50 value of 14 nM.

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

GSK429286A Chemical Structure

GSK429286A Chemical Structure

CAS No. : 864082-47-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
Estimated Time of Arrival: December 31
10 mg USD 168 In-stock
Estimated Time of Arrival: December 31
25 mg USD 288 In-stock
Estimated Time of Arrival: December 31
50 mg USD 504 In-stock
Estimated Time of Arrival: December 31
100 mg USD 720 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

GSK429286A is a selective inhibitor of ROCK1 with an IC50 value of 14 nM.

IC50 & Target

IC50: 14 nM (ROCK1)[1].

In Vitro

GSK429286A at 1 μM reduces ROCK2 activity over 20-fold, under conditions in which the only other kinase tested that is significantly inhibited is MSK1 whose activity is reduced ~5-fold. GSK429286A is a more selective ROCK2 inhibitor than the widely utilized ROCK inhibitor Y-27632 as assessed on kinase-specificity panel, and does not significantly inhibit LRRK2 even at doses as high as 30 μM (500-fold higher than IC50 of inhibition of ROCK2). GSK429286A slightly inhibits RSK and p70S6K with IC50 of 0.78 μM and 1.94 μM, respectively. GSK429286A significantly inhibits rat aortic ring dilation with IC50 of 190 nM[2].

In Vivo

GSK429286A has 61% oral bioavailability in male Sprague-Dawley rats. Oral administration of GSK429286A at single doses of 3-30 mg/kg dramatically reduces mean arterial pressure in the spontaneously hypertensive rats (SHRs) in a dose-dependent manner, with a maximum decrease of 50 mmHg after approximately 2 hours treatment at dose of 30 mg/kg[1].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 51 mg/mL (117.95 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3128 mL 11.5642 mL 23.1283 mL
5 mM 0.4626 mL 2.3128 mL 4.6257 mL
10 mM 0.2313 mL 1.1564 mL 2.3128 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Rats: Spontaneously hypertensive rats (SHRs) are treated with GSK429286A to establish its effect on mean arterial pressure. Compound is administered by single dose oral gavage (3, 10, 30 mg/kg)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

432.37

Formula

C₂₁H₁₆F₄N₄O₂

CAS No.

864082-47-3

SMILES

O=C(C(C(C1=CC=C(C(F)(F)F)C=C1)C2)=C(C)NC2=O)NC3=CC4=C(NN=C4)C=C3F

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.13%

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Product Name:
GSK429286A
Cat. No.:
HY-11000
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GSK429286A

Cat. No.: HY-11000