PERK Inhibitors
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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| S7307 | GSK2606414 | GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed. This compound impairs GANT-61 induced autophagy in NB cells with MYCN amplification. It exacerbates ER stress-induced apoptosis in HCT116 cells while reduces the apoptosis in SIL1 KD HeLa cells. |
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| S7033 | GSK2656157 | GSK2656157 is an ATP-competitive and highly selective inhibitor of PERK with IC50 of 0.9 nM in a cell-free assay, 500-fold greater against a panel of 300 kinases. This compound decreases apoptosis and inhibits excessive autophagy. |
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| S7400 | ISRIB (trans-isomer) | ISRIB (trans-isomer) is a potent and selective PERK inhibitor with IC50 of 5 nM and does not have global effects on translation, transcription, or mRNA stability in non-stressed cells. |
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| E1761 | AMG PERK 44 | AMG PERK 44 is a highly selective and orally active inhibitor of PERK with an IC50 of 6 nM. This compound exhibits 1000-fold and 160-fold selectivity over GCN2 and B-Raf, respectively. | ||
| E7772 | Ulixertinib hydrochloride | Ulixertinib hydrochloride (BVD-523 hydrochloride, VRT752271 hydrochloride) is a highly selective, ATP-competitive, and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. It also reduces A375 cell proliferation with an IC50 of 180 nM and inhibits phosphorylated ERK (pERK) and the downstream kinase RSK (pRSK) in the A375 melanoma cell line, with IC50 values of 4.1 μM and 0.14 μM, respectively. |
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