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GSK 429286

Cat. No. 3726

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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.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

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Safety Data Sheet: View Safety Data Sheet

References

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

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

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Extracellular Matrix and Adhesion Molecules Kinases

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