PERK
Inhibitory Selectivity
PERK Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7307 |
GSK2606414GSK2606414 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. |
Representative westerns and summary results showing decreased eIf2α phospho-immunoreactivity (Phos) following intracerebroventricular administration of GSK2606414 (or vehicle) to uninjured mice (n = 4/group). The total levels of eIF2α did not change as a result of treatment. When calculated as a phospho–total ratio (P/T), a significant decrease in phosphorylation was observed in mice treated with GSK2606414. *p < 0.05 between vehicle and drug-treated animals.
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| S7033 |
GSK2656157GSK2656157 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 inhibits excessive autophagy in kri1lcas002 HSPCs. Representative confocal images of mCherry-Lc3 puncta (autophagosomes) in kri1lcas002 mutant embryos in Tg (cmyb: egfp) transgenic background are shown. Scale bars, 5 μm.
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| 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. |
PERK inhibitor treatment restores female development in zar1 homozygous mutants. Juveniles were treated with two PERK inhibitors from 22 dpf to 60 dpf. Final concentration: ISRIB, 50 nM. **P<0.01, ***P<0.001.
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| S2923 |
SalubrinalSalubrinal is a selective inhibitor of eIF2α dephosphorylation and inhibits ER stress-mediated apoptosis with EC50 of ~15 μM in a cell-free assay. |
AngII (30 minutes)-induced Akt activation was attenuated by the ER stress inhibitors 4-PBA (5 mM, 2 hours), TUDCA (300 µg/ml, 1 hour), and salubrinal (30 µM, 1 hour) (n=5; *P<0.01 versus con, #P<0.05 versus Ang) |
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| S7437 |
Sal003Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor. |
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| S8304 |
AzoramideAzoramide 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. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7307 |
GSK2606414GSK2606414 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. |
Representative westerns and summary results showing decreased eIf2α phospho-immunoreactivity (Phos) following intracerebroventricular administration of GSK2606414 (or vehicle) to uninjured mice (n = 4/group). The total levels of eIF2α did not change as a result of treatment. When calculated as a phospho–total ratio (P/T), a significant decrease in phosphorylation was observed in mice treated with GSK2606414. *p < 0.05 between vehicle and drug-treated animals.
|
|
| S7033 |
GSK2656157GSK2656157 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 inhibits excessive autophagy in kri1lcas002 HSPCs. Representative confocal images of mCherry-Lc3 puncta (autophagosomes) in kri1lcas002 mutant embryos in Tg (cmyb: egfp) transgenic background are shown. Scale bars, 5 μm.
|
|
| 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. |
PERK inhibitor treatment restores female development in zar1 homozygous mutants. Juveniles were treated with two PERK inhibitors from 22 dpf to 60 dpf. Final concentration: ISRIB, 50 nM. **P<0.01, ***P<0.001.
|
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S2923 |
SalubrinalSalubrinal is a selective inhibitor of eIF2α dephosphorylation and inhibits ER stress-mediated apoptosis with EC50 of ~15 μM in a cell-free assay. |
AngII (30 minutes)-induced Akt activation was attenuated by the ER stress inhibitors 4-PBA (5 mM, 2 hours), TUDCA (300 µg/ml, 1 hour), and salubrinal (30 µM, 1 hour) (n=5; *P<0.01 versus con, #P<0.05 versus Ang) |
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| S7437 |
Sal003Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor. |
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| S8304 |
AzoramideAzoramide 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. |
