PERK

Choose Selective PERK Inhibitors

PERK Products

  • All (8)
  • PERK Inhibitors (3)
  • PERK Activators (2)
  • PERK Modulators (3)
  • New PERK Products
Catalog No. Product Name Information Product Use Citations Product Validations
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. GSK2656157 decreases apoptosis and inhibits excessive autophagy.
Nat Immunol, 2022, 23(3):431-445
Nat Cell Biol, 2022, 24(5):766-782
Front Cell Dev Biol, 2021, 9:769213
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. GSK2606414 impairs GANT-61 induced autophagy in NB cells with MYCN amplification. GSK2606414 exacerbates ER stress-induced apoptosis in HCT116 cells while reduces the apoptosis in SIL1 KD HeLa cells.
Nat Cell Biol, 2022, 24(5):766-782
Adv Sci (Weinh), 2022, e2105469
Cell Rep, 2022, 38(10):110490
S7400 ISRIB (trans-isomer) ISRIB (trans-isomer), the trans-isomer of ISRIB, 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.
Clin Cancer Res, 2020, 10.1158/1078-0432.CCR-19-1900
Cell Death Dis, 2020, 6;11(1):17
Cell Stem Cell, 2019, 25(5):639-653
E1030New CCT020312

CCT020312 is a selective PERK (EIF2AK3) activator with an EC50 of 5.1 μM. CCT020312 can be used for the selective activation of EIF2A-mediated translation control.

S0006 BTdCPU BTdCPU is a potent activator of heme regulated inhibitor kinase (HRI), one of eukaryotic translation initiation factor 2α kinases (eIF2α-kinases).
Front Cell Dev Biol, 2021, 9:675486
S2923 Salubrinal Salubrinal is a selective inhibitor of eIF2α dephosphorylation and inhibits ER stress-mediated apoptosis with EC50 of ~15 μM in a cell-free assay.
Oncogene, 2022, 10.1038/s41388-022-02328-4
Nat Commun, 2021, 12(1):1589
Cell Mol Life Sci, 2021, 10.1007/s00018-021-03970-z
S7437 Sal003 Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor.
S8304 Azoramide Azoramide is a small-molecule modulator of the unfolded protein response (UPR). It improves ER protein-folding ability and activates ER chaperone capacity to protect cells against ER stress.
Stem Cell Res, 2022, 60:102686
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. GSK2656157 decreases apoptosis and inhibits excessive autophagy.
Nat Immunol, 2022, 23(3):431-445
Nat Cell Biol, 2022, 24(5):766-782
Front Cell Dev Biol, 2021, 9:769213
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. GSK2606414 impairs GANT-61 induced autophagy in NB cells with MYCN amplification. GSK2606414 exacerbates ER stress-induced apoptosis in HCT116 cells while reduces the apoptosis in SIL1 KD HeLa cells.
Nat Cell Biol, 2022, 24(5):766-782
Adv Sci (Weinh), 2022, e2105469
Cell Rep, 2022, 38(10):110490
S7400 ISRIB (trans-isomer) ISRIB (trans-isomer), the trans-isomer of ISRIB, 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.
Clin Cancer Res, 2020, 10.1158/1078-0432.CCR-19-1900
Cell Death Dis, 2020, 6;11(1):17
Cell Stem Cell, 2019, 25(5):639-653
E1030New CCT020312

CCT020312 is a selective PERK (EIF2AK3) activator with an EC50 of 5.1 μM. CCT020312 can be used for the selective activation of EIF2A-mediated translation control.

S0006 BTdCPU BTdCPU is a potent activator of heme regulated inhibitor kinase (HRI), one of eukaryotic translation initiation factor 2α kinases (eIF2α-kinases).
Front Cell Dev Biol, 2021, 9:675486
S2923 Salubrinal Salubrinal is a selective inhibitor of eIF2α dephosphorylation and inhibits ER stress-mediated apoptosis with EC50 of ~15 μM in a cell-free assay.
Oncogene, 2022, 10.1038/s41388-022-02328-4
Nat Commun, 2021, 12(1):1589
Cell Mol Life Sci, 2021, 10.1007/s00018-021-03970-z
S7437 Sal003 Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor.
S8304 Azoramide Azoramide is a small-molecule modulator of the unfolded protein response (UPR). It improves ER protein-folding ability and activates ER chaperone capacity to protect cells against ER stress.
Stem Cell Res, 2022, 60:102686
E1030New CCT020312

CCT020312 is a selective PERK (EIF2AK3) activator with an EC50 of 5.1 μM. CCT020312 can be used for the selective activation of EIF2A-mediated translation control.

Tags: PERK inhibitor|PERK agonist|PERK activator|PERK inducer|PERK antagonist|PERK signaling pathway|PERK assay kit