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 inhibitor

Salubrinal is a cell-permeable, selective inhibitor of cellular phosphatase complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit α (eIF2α). Protects cells from endoplasmic reticulum stress-induced apoptosis (EC50 ~ 15 μM). Learn More

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 inhibitor

GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM. Learn More

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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 Inhibitor

GSK2656157 is an ATP-competitive inhibitor of PERK enzyme activity with an IC(50) of 0.9 nmol/L. It is highly selective for PERK with IC(50) values >100 nmol/L against a panel of 300 kinases. Learn More

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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 inhibitor

ISRIB (trans-isomer) is a potent and selective small molecule inhibitor of PERK signaling (IC50 ~5 nM) that can potently reverse the effects of eIF2α phosphorylation. Learn More

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ISRIB

Catalog No. A14302
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PERK inhibitor

ISRIB is a potent and selective PERK inhibitor with IC50 of 5 nM. Learn More

Product Citations (2)

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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
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Azoramide

Catalog No. A16075
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UPR modulator

Azoramide is a small-molecule modulator of the unfolded protein response with antidiabetic activity. Learn More

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CCT020312

Catalog No. A19137
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EIF2AK3/PERK activator

CCT020312 is a selective EIF2AK3/PERK activator. CCT020312 elicits EIF2A phosphorylation in cells. Learn More

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