GSK2656157 (Cat No.:I001285) is an ATP-competitive inhibitor that specifically targets the enzyme activity of PERK (protein kinase RNA-like endoplasmic reticulum kinase). It displays a potent inhibitory effect on PERK with an IC50 of 0.9 nM. Importantly, GSK2656157 exhibits high selectivity for PERK, as it has IC50 values greater than 100 nM when tested against a panel of 300 kinases. This selectivity profile suggests that GSK2656157 has minimal off-target effects on other kinases. The inhibition of PERK by GSK2656157 provides a valuable tool for studying PERK-mediated cellular processes and has potential therapeutic applications in diseases associated with PERK dysregulation, such as cancer and neurodegenerative disorders.
| Catalog Number | I001285 |
| CAS Number | 1337532-29-2 |
| Synonyms | 1-(5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoroindolin-1-yl)-2-(6-methylpyridin-2-yl)ethanone |
| Molecular Formula | C23H21FN6O |
| Purity | ≥95% |
| Target | PERK |
| Solubility | DMSO: ≥ 41 mg/mL |
| Storage | Store at -20 C |
| IC50 | 0.9 nM |
| IUPAC Name | 1-[5-(4-amino-7-methylpyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoro-2,3-dihydroindol-1-yl]-2-(6-methylpyridin-2-yl)ethanone |
| InChI | InChI=1S/C23H21FN6O/c1-13-4-3-5-14(28-13)10-19(31)30-9-8-16-18(30)7-6-15(21(16)24)17-11-29(2)23-20(17)22(25)26-12-27-23/h3-7,11-12H,8-10H2,1-2H3,(H2,25,26,27) |
| InChIKey | PRWSIEBRGXYXAJ-UHFFFAOYSA-N |
| SMILES | CC1=NC(=CC=C1)CC(=O)N2CCC3=C2C=CC(=C3F)C4=CN(C5=C4C(=NC=N5)N)C |
| Reference | <br /> |
