| Name | GSK 2606414 |
|---|---|
| Supplier | Tocris Bioscience |
| Catalog | 4143 |
| Prices | $245.00, $1,005.00 |
| Sizes | 10 mg, 50 mg |
| Function Type | Inhibitor |
| Cas Number | 1337531-36-8 |
| Chemical Name | 1-[5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-2,3-dihydro-1H-indol-1-yl]-2-[3-(trifluoromethyl)phenyl]ethanone |
| Formula | C24H20F3N5O |
| Molecular Weight | 451.44 |
| Purity | >99 % |
| Description | Potent and selective protein kinase R-like ER kinase (PERK) inhibitor (IC 50 = 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. |
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Axten JM, Medina JR, Feng Y, Shu A, Romeril SP, Grant SW, Li WH, Heerding DA, Minthorn E, Mencken T, Atkins C, Liu Q, Rabindran S, Kumar R, Hong X, Goetz A, Stanley T, Taylor JD, Sigethy SD, Tomberlin GH, Hassell AM, Kahler KM, Shewchuk LM, Gampe RT. J Med Chem. 2012 Aug 23;55(16):7193-207.
Harding HP, Zyryanova AF, Ron D. J Biol Chem. 2012 Dec 28;287(53):44338-44.