| 货号 | 5107/50 |
| 别名 | 1-[5-(4-Amino-7-methyl-7H-pyrrolo[2 |
| 供应商 | Tocris |
| 生物活性 | Potent and selective protein kinase R-like ER kinase (PERK) inhibitor (IC50 = 0.4 nM). Exhibits >1000-fold selectivity for PERK over HR1 and PKR. Inhibits thapsigargin-induced PERK phosphorylation in lung carcinoma A549 cells. Attenuates subcutaneous pancreatic human tumor xenograft growth in mice. Orally bioavailable. |
| 运输条件 | Blue Ice |
| 存放说明 | -20℃ |
| 纯度 | >99 % |
| 计算分子量 | 451.44 |
| 分子式 | C24H20F3N5 |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO |
| 参考文献 | Axtenet al (2012) Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK). J.Med.Chem. 55 7193. PMID: 22827572. Hardinget al (2012) Uncoupling proteostasis and development in vitro with a small molecule inhibitor of the pancreatic endoplasmic reticulum kinase, PERK. J.Biol.Chem. 287 44338. PMID: 23148209. |