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Chemical Structure : GSK-2656157
CAS No.: 1337532-29-2
Catalog No.: PC-49643Not For Human Use, Lab Use Only.
GSK2656157 (GSK 2656157) is a potent, selective and ATP-competitive inhibitor of PERK with biochemical IC50 of 0.9 nM and cellular p-PERK IC50 of 30 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $128 | In stock | |
| 25 mg | $218 | In stock | |
| 50 mg | $368 | In stock | |
| 100 mg | Get quote |
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GSK2656157 (GSK 2656157) is a potent, selective and ATP-competitive inhibitor of PERK with biochemical IC50 of 0.9 nM and cellular p-PERK IC50 of 30 nM.
GSK2656157 shows selectivity (>500-fold) over HRI, PKR, and GCN2, other members of the EIF2AK family, and high IC50 values (>100 nM) against a panel of 300 kinases.
GSK2656157 inhibits stress-induced PERK autophosphorylation, eIF2α substrate phosphorylation, together with corresponding decreases in ATF4 and CAAT/enhancer binding protein homologous protein (CHOP) in multiple cell lines.
Oral administration of GSK2656157 to mice shows a dose- and time-dependent pharmacodynamic response in pancreas as measured by PERK autophosphorylation.
GSK2656157 exhibited antitumor effect in multiple human tumor xenografts growth in mice.
| M.Wt | 416.45 | |
| Formula | C23H21FN6O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
1-[5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoro-2,3-dihydro-1H-indol-1-yl]-2-(6-methyl-2-pyridinyl)ethanone |
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1. Atkins C, et al. Cancer Res. 2013 Mar 15;73(6):1993-2002.
2. Krishnamoorthy J, et al. Cell Cycle. 2014;13(5):801-6.
3. Axten JM, et al. ACS Med Chem Lett. 2013 Aug 12;4(10):964-8.
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