GSK 429286
Chemical Name: 4-[4-(Trifluoromethyl)phenyl]-N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-1,4,5,6-tetrahydro-3-pyridinecarboxamide
Purity: ≥97%
Biological Activity
GSK 429286 is a selective Rho-kinase inhibitor (IC50 values are 14, 780 and 1940 nM for ROCK1, RSK and p70S6K respectively). Reverses adrenaline-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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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Development of dihydropyridone indazole amides as selective rho-kinase inhibitors.
Goodman et al.
J.Med.Chem., 2007;50:6 -
Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson's disease.
Nichols et al.
Biochem.J., 2009;424:47
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Citations for GSK 429286
The citations listed below are publications that use Tocris products. Selected citations for GSK 429286 include:
4 Citations: Showing 1 - 4
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Unexpected PD-L1 immune evasion mechanism in TNBC, ovarian, and other solid tumors by DR5 agonist antibodies.
Authors: J Chuck Et al.
EMBO Mol Med 2021;13:e12716
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Phospho-substrate profiling of Epac-dependent protein kinase C activity.
Authors: Diana J Et al.
Mol Cell Biochem 2019;456:167-178
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RhoD Inhibits RhoC-ROCK-Dependent Cell Contraction via PAK6.
Authors: Durkin Et al.
Dev Cell 2017;41:315
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Neural Precursor-Derived Pleiotrophin Mediates Subventricular Zone Invasion by Glioma.
Authors: Qin Et al.
Cell 2017;170:845
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