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Submit ReviewGSK 429286
说明： Selective Rho-kinase (ROCK) inhibitor
别名： GSK429286A
化学名： 4-[4-(Trifluoromethyl)phenyl]-N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-1,4,5,6-tetrahydro-3-pyridinecarboxamide
纯度： ≥97% (HPLC)
生物活性 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.
许可信息
Sold for research purposes under agreement from GlaxoSmithKline
化合物库 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. 了解 Tocris 化合物库的更多信息。
技术数据 for GSK 429286
| 分子量 | 432.37 |
| 公式 | C21H16F4N4O2 |
| 储存 | Store at +4°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for GSK 429286
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 43.24 | 100 | |
| ethanol | 10.81 | 25 |
制备储备液 for GSK 429286
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for GSK 429286
参考文献 for GSK 429286
参考文献是支持产品生物活性的出版物。
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.
按产品操作查看相关产品
关键词: 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 篇 GSK 429286 的引用文献
引用文献是使用了 Tocris 产品的出版物。 GSK 429286 的部分引用包括：
Diana J et al (2019) Phospho-substrate profiling of Epac-dependent protein kinase C activity. Mol Cell Biochem 456 167-178 PMID: 30739223
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
Qin et al (2017) Neural Precursor-Derived Pleiotrophin Mediates Subventricular Zone Invasion by Glioma. Cell 170 845 PMID: 28823557
Durkin et al (2017) RhoD Inhibits RhoC-ROCK-Dependent Cell Contraction via PAK6. Dev Cell 41 315 PMID: 28486133
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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