GSK 429286

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Cat.No. 3726 - GSK 429286 | C21H16F4N4O2 | CAS No. 864082-47-3
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)
Datasheet
Citations
Literature

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

Compound Libraries

GSK 429286 is also offered as part of the Tocriscreen Plus and Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 432.37. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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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View all Rho-Kinases Inhibitors

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

Citations for GSK 429286

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Pathways for GSK 429286

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