PERK

PERK製品

• All (10)
• PERK阻害剤 (4)
• PERK活性剤(3)
• PERKモジュレータ(3)
• 新製品

製品コード	製品名称	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
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.	Cell, 2024, 187(14):3652-3670.e40 Autophagy, 2024, 1-22. Exp Mol Med, 2024, 56(2):408-421.
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.	Cancer Gene Ther, 2024, 10.1038/s41417-024-00818-z Int J Mol Sci, 2024, 25(5)2611 Respir Res, 2024, 25(1):201
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 Death Dis, 2024, 15(1):31 Respir Res, 2024, 25(1):201 Cell Genom, 2024, 4(2):100487
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.	J Biol Chem, 2022, S0021-9258(22)01264-9 Clin Cancer Res, 2020, 10.1158/1078-0432.CCR-19-1900 Cell Death Dis, 2020, 6;11(1):17
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.	PeerJ, 2024, 12:e16844 J Adv Res, 2022, S2090-1232(22)00149-7 Stem Cell Res, 2022, 60:102686
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. CCT020312 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
E1761New	AMG PERK 44	AMG PERK 44 is a highly selective and orally active inhibitor of PERK with an IC50 of 6 nM. AMG PERK 44 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. MK-28 exhibits an IC50 ~3-fold higher than CCT020312 in rescuing mutant huntingtin protein (mHtt)-expressing striatal neurons from apoptosis. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice.
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.	Cell, 2024, 187(14):3652-3670.e40 Autophagy, 2024, 1-22. Exp Mol Med, 2024, 56(2):408-421.
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.	Cancer Gene Ther, 2024, 10.1038/s41417-024-00818-z Int J Mol Sci, 2024, 25(5)2611 Respir Res, 2024, 25(1):201
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.	J Biol Chem, 2022, S0021-9258(22)01264-9 Clin Cancer Res, 2020, 10.1158/1078-0432.CCR-19-1900 Cell Death Dis, 2020, 6;11(1):17
E1761New	AMG PERK 44	AMG PERK 44 is a highly selective and orally active inhibitor of PERK with an IC50 of 6 nM. AMG PERK 44 exhibits 1000-fold and 160-fold selectivity over GCN2 and B-Raf, respectively.
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. CCT020312 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
S6952	MK-28	MK-28 is a potent and selective activator of PERK. MK-28 exhibits an IC50 ~3-fold higher than CCT020312 in rescuing mutant huntingtin protein (mHtt)-expressing striatal neurons from apoptosis. MK-28 exhibits remarkable pharmacokinetic properties and high BBB penetration in mice.
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 Death Dis, 2024, 15(1):31 Respir Res, 2024, 25(1):201 Cell Genom, 2024, 4(2):100487
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.	PeerJ, 2024, 12:e16844 J Adv Res, 2022, S2090-1232(22)00149-7 Stem Cell Res, 2022, 60:102686
E1761New	AMG PERK 44	AMG PERK 44 is a highly selective and orally active inhibitor of PERK with an IC50 of 6 nM. AMG PERK 44 exhibits 1000-fold and 160-fold selectivity over GCN2 and B-Raf, respectively.