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

GSK429286A 

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

GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 values of 14 nM and 63 nM, respectively.

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 $88 In-stock
5 mg $80 In-stock
10 mg $140 In-stock
25 mg $240 In-stock
50 mg $420 In-stock
100 mg $600 In-stock
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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 values of 14 nM and 63 nM, respectively.

IC50 & Target

IC50: 14 nM (ROCK1), 63 nM(ROCK2)[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].

References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
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

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

Solvent & Solubility

DMSO: ≥ 51 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.13%

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