GSK 429286

Cat. No. 3726

GSK 429286 C21H16F4N4O2 [864082-47-3]

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Alternative Name: GSK429286A

Chemical Name: 4-[4-(Trifluoromethyl)phenyl]-N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-1,4,5,6-tetrahydro-3-pyridinecarboxamide

Biological Activity

Selective Rho-kinase inhibitor (IC50 values are 14, 780 and 1940 nM for ROCK1, RSK and p70S6K respectively). Reverses adrenalin-induced contraction of the rat aortic ring (IC50 = 190 nM) and causes a dose-dependent decrease in mean arterial blood pressure in spontaneous hypertensive rats. Orally active.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Technical Data

M.Wt:
432.37
Formula:
C21H16F4N4O2
Solubility:
Soluble to 100 mM in DMSO and to 25 mM in ethanol
Purity:
>97 %
Storage:
Store at +4°C
CAS No:
864082-47-3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Nichols et al (2009) Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson's disease. Biochem.J. 424 47. PMID: 19740074.

Goodman et al (2007) Development of dihydropyridone indazole amides as selective rho-kinase inhibitors. J.Med.Chem. 50 6. PMID: 17201405.

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Keywords: GSK 429286, supplier, Selective, Rho-kinases, ROCK, inhibitors, inhibits, Rho-Associated, Coiled-Coil, Kinases, p160ROCK, ROK, GSK429286, GlaxoSmithKline, GSK, GSK429286A, Tocris Bioscience, Rho-Kinases Inhibitor products

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