GSK429286A

For research use only.

Catalog No.S1474 Synonyms: RHO-15

20 publications

GSK429286A Chemical Structure

CAS No. 864082-47-3

GSK429286A (RHO-15) is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.

Selleck's GSK429286A has been cited by 20 publications

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Biological Activity

Description GSK429286A (RHO-15) is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.
Features Greater selectivity than Y-27632.
Targets
ROCK1 [1]
(Cell-free assay)
ROCK2 [2]
(Cell-free assay)
14 nM 63 nM
In vitro

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. [1] 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). Like GSK269962A but not sunitinib, GSK429286A treatment at 10 μM ablates basal or G14V-Rho mutant induced phosphorylation of MYPT at Thr850 in HEK-293 cells to a similar extent as H-1152 and Y-27632, consistent with ROCK mediating this phosphorylation, whereas GSK429286A does not inhibit ERM protein phosphorylation either in the presence or absence of G14V-Rho. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 cells Mly1SpVv[3Srb36gZZN{[Xl? M{TUTmlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUl;DT|Eh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDheEAyOCCvTTygTWM2OD1yLkCxOEDPxE1? M1;XRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5MkCxOFA2Lz5zN{KwNVQxPTxxYU6=

... Click to View More Cell Line Experimental Data

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]

Protocol

Animal Research:[1]
- Collapse
  • Animal Models: Male spontaneously hypertensive rats (SHRs)
  • Dosages: ~30 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 87 mg/mL (201.21 mM)
Ethanol 4 mg/mL (9.25 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
15% Captisol+citrate vehicle
For best results, use promptly after mixing.
15 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 432.37
Formula

C21H16F4N4O2

CAS No. 864082-47-3
Storage powder
in solvent
Synonyms RHO-15
Smiles CC1=C(C(CC(=O)N1)C2=CC=C(C=C2)C(F)(F)F)C(=O)NC3=C(C=C4C(=C3)C=NN4)F

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    The product sold by Selleckchem has an “A” at the end. I am wondering if GSK429286A is the same compound as GSK429286?

  • Answer:

    For the compound GSK429286A and GSK429286, they are the same comopund and have a identical CAS# (864082-47-3). Attached please find the reference about GSK429286A, which published by GSK, and the link is followed: http://www.ncbi.nlm.nih.gov/pubmed/19740074.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID