PERK
- Inhibitory Selectivity
- Solubility
| Catalog No. | Product Name | Solubility(25°C) | ||
|---|---|---|---|---|
| Water | DMSO | Alcohol | ||
| S7307 | GSK2606414 | <1 mg/mL | 90 mg/mL | 19 mg/mL |
| S7033 | GSK2656157 | <1 mg/mL | 32 mg/mL | <1 mg/mL |
| S7400 | ISRIB (trans-isomer) | <1 mg/mL | 4 mg/mL | <1 mg/mL |
| S2923 | Salubrinal | <1 mg/mL | 95 mg/mL | 2 mg/mL |
| S7437 | Sal003 | <1 mg/mL | 93 mg/mL | <1 mg/mL |
| S8304 | Azoramide | <1 mg/mL | 61 mg/mL | 61 mg/mL |
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. |
C. PERK inhibitor (PERKi, GSK2606414) partially reverted vemurafenib-induced autophagy. BCPAP cells were treated with 5 M PLX and/or 1 M PERKi for 24 hours. After that, protein lysates were prepared and subjected to immunoblotting against the indicated antibodies. Relative quantity of LC3II/LC3I was calculated by ImageJ densitometric analysis and normalized to control (DMSO/DMSO PERKi).
|
|
| 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.
|
|
| 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) |
|
| S7437 |
Sal003Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor. |
||
| 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. |
C. PERK inhibitor (PERKi, GSK2606414) partially reverted vemurafenib-induced autophagy. BCPAP cells were treated with 5 M PLX and/or 1 M PERKi for 24 hours. After that, protein lysates were prepared and subjected to immunoblotting against the indicated antibodies. Relative quantity of LC3II/LC3I was calculated by ImageJ densitometric analysis and normalized to control (DMSO/DMSO PERKi).
|
|
| 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. |
2014, 10.1681/ASN.2013121332 2018, 62(8):e1700890 2017, 6(5):e341 |
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) |
| S7437 |
Sal003Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor. |
||
| 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. |
