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Submit ReviewGSK 429286
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)
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.
Product Datasheets for GSK 429286
References for GSK 429286
References are publications that support the biological activity of the product.
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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Keywords: GSK 429286, GSK 429286 supplier, Selective, Rho-kinases, ROCK, inhibitors, inhibits, Rho-Associated, Coiled-Coil, Kinases, p160ROCK, ROK, GSK429286, GlaxoSmithKline, GSK, GSK429286A, 3726, Tocris Bioscience
4 Citations for GSK 429286
Citations are publications that use Tocris 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
Diana J et al (2019) Phospho-substrate profiling of Epac-dependent protein kinase C activity. Mol Cell Biochem 456 167-178 PMID: 30739223
Qin et al (2017) Neural Precursor-Derived Pleiotrophin Mediates Subventricular Zone Invasion by Glioma. Cell 170 845 PMID: 28823557
J Chuck et al (2021) Unexpected PD-L1 immune evasion mechanism in TNBC, ovarian, and other solid tumors by DR5 agonist antibodies. EMBO Mol Med 13 e12716 PMID: 33587338
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Stem Cells Scientific Review
Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.
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Stem cells have potential as a source of cells and tissues for research and treatment of disease. This poster summarizes some key protocols demonstrating the use of small molecules across the stem cell workflow, from reprogramming, through self-renewal, storage and differentiation to verification. Advantages of using small molecules are also highlighted.
Stem Cells Poster
Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.