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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.
Solubility Data 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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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
If you know of a relevant reference for GSK 429286, please let us know.
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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:
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
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
Do you know of a great paper that uses GSK 429286 from Tocris? Please let us know.
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Literature in this Area
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