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PERK
PERK Products
- All (12)
- PERK Inhibitors (5)
- PERK Activators (3)
- PERK Modulators (3)
- New PERK Products
| Catalog 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. 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. |
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| 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. |
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| 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. |
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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. |
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| 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. | ||
| S0006 | BTdCPU | BTdCPU is a potent activator of heme regulated inhibitor kinase (HRI), one of eukaryotic translation initiation factor 2α kinases (eIF2α-kinases). | ||
| 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. |
||
| F0027New | PERK Rabbit mAb | PERK,p-ERK | ||
| E7772New | Ulixertinib hydrochloride | Ulixertinib hydrochloride (BVD-523 hydrochloride, VRT752271 hydrochloride) is a highly selective, ATP-competitive, and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. It also reduces A375 cell proliferation with an IC50 of 180 nM and inhibits phosphorylated ERK (pERK) and the downstream kinase RSK (pRSK) in the A375 melanoma cell line, with IC50 values of 4.1 μM and 0.14 μM, respectively. | ||
| E1761 | 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| E7772New | Ulixertinib hydrochloride | Ulixertinib hydrochloride (BVD-523 hydrochloride, VRT752271 hydrochloride) is a highly selective, ATP-competitive, and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. It also reduces A375 cell proliferation with an IC50 of 180 nM and inhibits phosphorylated ERK (pERK) and the downstream kinase RSK (pRSK) in the A375 melanoma cell line, with IC50 values of 4.1 μM and 0.14 μM, respectively. | ||
| E1761 | 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). | ||
| 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. |
||
| 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. |
|
|
| 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. | ||
| F0027New | PERK Rabbit mAb | PERK,p-ERK | ||
| E7772New | Ulixertinib hydrochloride | Ulixertinib hydrochloride (BVD-523 hydrochloride, VRT752271 hydrochloride) is a highly selective, ATP-competitive, and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. It also reduces A375 cell proliferation with an IC50 of 180 nM and inhibits phosphorylated ERK (pERK) and the downstream kinase RSK (pRSK) in the A375 melanoma cell line, with IC50 values of 4.1 μM and 0.14 μM, respectively. |
Choose Selective PERK Inhibitors
Tags: PERK inhibitor|PERK agonist|PERK activator|PERK inducer|PERK antagonist|PERK signaling pathway|PERK assay kit
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