PERK

Inhibitory Selectivity

Catalog No.	Inhibitor Name	PERK	Other
A12792	GSK2606414	****	EIF2AK1 (HRI),EIF2AK2 (PKR)
A13577	GSK2656157	***
A13816	ISRIB (trans-isomer)	**
A12676	Salubrinal

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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Salubrinal

Catalog No. A12676
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eIF2α dephosphorylation 抑制剂

Salubrinal是细胞磷酸酶复合物的可渗透细胞的选择性抑制剂，可将真核翻译起始因子2亚基α（eIF2α）磷酸化。保护细胞免受内质网应激诱导的细胞凋亡（EC50?15 μM）。了解更多

Product Citations (1)

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- Gregory R. Kardos, .et al. Salubrinal in Combination With 4E1RCat Synergistically Impairs Melanoma Development by Disrupting the Protein Synthetic Machinery, Front Oncol, 2020, 10: 834 PMID: 32637352
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GSK2606414

Catalog No. A12792
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PERK 抑制剂

GSK2606414是口服有效的选择性PERK抑制剂，IC50为0.4 nM。了解更多

Product Citations (2)

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- Linhao Xu, .et al. Suppression of CHOP Reduces Neuronal Apoptosis and Rescues Cognitive Impairment Induced by Intermittent Hypoxia by Inhibiting Bax and Bak Activation, Neural Plasticity, 2021, 23 Aug
- Takashi Shimizu, .et al. PERK inhibition attenuates vascular remodeling in pulmonary arterial hypertension caused by BMPR2 mutation, Sci Signal, 2021, Jan 26;14(667):eabb3616 PMID: 33500333
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GSK2656157

Catalog No. A13577
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PERK 抑制剂

GSK2656157是PERK酶活性的ATP竞争性抑制剂，IC50为0.9 nmol/L。对于PER（K）IC50值> 100 nmol/L，对300种激酶组合具有高度选择性。了解更多

Product Citations (2)

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- Cao W, .et al. Hoxa5 alleviates obesity‐induced chronic inflammation by reducing ER stress and promoting M2 macrophage polarization in mouse adipose tissue, J Cell Mol Med, 2019, Aug 23 PMID: 31441588
- Kosuke Ishikawa, .et al. A highly sensitive trap vector system for isolating reporter cells and identification of responsive genes, Biology Methods and Protocols, 2018, 1–10
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ISRIB (trans-isomer)

Catalog No. A13816
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PERK 抑制剂

ISRIB (trans-isomer)是一种有效的选择性小分子PERK信号抑制剂（IC50?5 nM），可以有效逆转eIF2α磷酸化的作用。了解更多

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ISRIB

Catalog No. A14302
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PERK 抑制剂

ISRIB是一种有效的选择性PERK抑制剂，IC50为5 nM。了解更多

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- Satoshi Watanabe, .et al. Resetting proteostasis with ISRIB promotes epithelial differentiation to attenuate pulmonary fibrosis, Proc Natl Acad Sci U S A, 2021, May 18;118(20) PMID: 33972447
- Satoshi Watanabe, .et al. Resetting proteostasis with ISRIB prevents pulmonary fibrosis, bioRxiv, 2020, February 27