GSK 429286

Name: GSK 429286
Brand: Tocris Bioscience
SKU: 3726

Tocris Bioscience a Bio-Techne Brand

Catalog # 3726

Citations (2)

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Key Product Details

Description:	Selective Rho-kinase (ROCK) inhibitor
Alternative Names:	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
Purity:	≥97% (HPLC)
Molecular Weight:	432.37

View Full Technical Details for GSK 429286

Biological Activity for GSK 429286

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.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Compound Libraries for GSK 429286

GSK 429286 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.

Technical Data for GSK 429286

M. Wt	432.37
Formula	C₂₁H₁₆F₄N₄O₂
Storage	Store at +4°C
Purity	≥97% (HPLC)
CAS Number	864082-47-3
PubChem ID	11373846
InChi Key	OLIIUAHHAZEXEX-UHFFFAOYSA-N
Smiles	O=C1CC(C2=CC=C(C(F)(F)F)C=C2)C(C(NC3=C(F)C=C(NN=C4)C4=C3)=O)=C(C)N1

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.

Solubility for GSK 429286

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	43.24	100
	ethanol	10.81	25

Preparing Stock Solutions for GSK 429286

The following data is based on the product molecular weight 432.37.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.31 mL	11.56 mL	23.13 mL
5 mM	0.46 mL	2.31 mL	4.63 mL
10 mM	0.23 mL	1.16 mL	2.31 mL
50 mM	0.05 mL	0.23 mL	0.46 mL

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References for GSK 429286

References are publications that support the biological activity of the product.

Nichols Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson's disease. Biochem.J. 2009 PMID: 19740074
Goodman Development of dihydropyridone indazole amides as selective rho-kinase inhibitors. J.Med.Chem. 2007 PMID: 17201405

Citations for GSK 429286 (2)

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Citations are publications that use Bio-Techne products. Selected citations for GSK 429286 include:

Durkin et al. (2017) RhoD Inhibits RhoC-ROCK-Dependent Cell Contraction via PAK6. Dev Cell. 41:315
PMID: 28486133
Qin et al. (2017) Neural Precursor-Derived Pleiotrophin Mediates Subventricular Zone Invasion by Glioma. Cell. 170:845
PMID: 28823557

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