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PERK

Other ER stress & UPR Related Inhibitors

IRE1 PDI PKR ATF-6 ER stress
Cat.No. Product Name Information Product Use Citations Product Validations
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.
Immunity, 2025, 58(10):2489-2504.e8
J Transl Med, 2025, 23(1):860
Biomolecules, 2025, 15(1)76
Verified customer review of GSK2606414
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.
EMBO J, 2025, 44(4):1107-1130
J Adv Res, 2025, S2090-1232(25)00385-6
J Clin Invest, 2024, 135(1)e179874
Verified customer review of GSK2656157
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.
Cell Discov, 2025, 11(1):80
Cell Metab, 2025, 37(8):1715-1731.e11
EMBO J, 2025, 44(4):1107-1130
Verified customer review of Salubrinal
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.
Life Sci Alliance, 2025, 8(3)e202302259
Int J Mol Sci, 2024, 25(19)10571
J Biol Chem, 2022, S0021-9258(22)01264-9
Verified customer review of ISRIB (trans-isomer)
S7437 Sal003 Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor.
Front Pharmacol, 2023, 14:1095307
bioRxiv, 2023, 2023.05.19.540602
bioRxiv, 2023, 2023.05.19.540602
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.
Nat Commun, 2025, 16(1):6247
PeerJ, 2024, 12:e16844
J Adv Res, 2022, S2090-1232(22)00149-7
S0006 BTdCPU BTdCPU is a potent activator of heme regulated inhibitor kinase (HRI), one of eukaryotic translation initiation factor 2α kinases (eIF2α-kinases).
EMBO Rep, 2024, 25(10):4488-4514
Front Cell Dev Biol, 2021, 9:675486
E1030 CCT020312

CCT020312 is a selective PERK (EIF2AK3) activator with an EC50 of 5.1 μM. This compound can be used for the selective activation of EIF2A-mediated translation control.
Int J Mol Sci, 2023, 24(21)15561
Int J Mol Med, 2023, 52(1)56
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.
S6952 MK-28 MK-28 is a potent and selective activator of PERK. This compound exhibits an IC50 ~3-fold higher than CCT020312 in rescuing mutant huntingtin protein (mHtt)-expressing striatal neurons from apoptosis. It exhibits remarkable pharmacokinetic properties and high BBB penetration in mice.