AMG PERK 44
Chemical Name: 4-[2-Amino-4-methyl-3-(2-methyl-6-quinolinyl)benzoyl]-1,2-dihydro-1-methyl-2,5-diphenyl-3H-pyrazol-3-one hydrochloride
Purity: ≥98%
Biological Activity
AMG PERK 44 is a potent and selective PERK inhibitor (IC50 = 6 nM). Exhibits >160-fold selectivity for PERK over B-Raf and GCN2, as well as a panel of 387 other kinases. Orally bioavailable.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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Discovery of 1H-pyrazol-3(2H)-ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK).
Smith et al.
J.Med.Chem., 2015;58:1426
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Citations for AMG PERK 44
The citations listed below are publications that use Tocris products. Selected citations for AMG PERK 44 include:
8 Citations: Showing 1 - 8
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The endoplasmic reticulum kinase PERK interacts with the oxidoreductase ERO1 to metabolically adapt mitochondria.
Authors: Roberto Et al.
Cell Rep 2023;42:111899
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Cholinergic neurons constitutively engage the ISR for dopamine modulation and skill learning in mice.
Authors: Viviana Et al.
Science 2021;372
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FOXO1 promotes HIV latency by suppressing ER stress in T cells.
Authors: Emilie Et al.
Nat Microbiol 2020;5:1144-1157
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The Unfolded Protein Response Mediator PERK Governs Myeloid Cell-Driven Immunosuppression in Tumors through Inhibition of STING Signaling.
Authors: Shikhar Et al.
Immunity 2020;52:668-682.e7
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Endorepellin evokes an angiostatic stress signaling cascade in endothelial cells.
Authors: Carolyn G Et al.
J Biol Chem 2020;295:6344-6356
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The unfolded protein response modulators GSK2606414 and KIRA6 are potent KIT inhibitors.
Authors: Mahameed Et al.
Cell Death Dis 2019;10:300
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The ER Stress Inducer l-Azetidine-2-Carboxylic Acid Elevates the Levels of Phospho-eIF2α and of LC3-II in a Ca2+-Dependent Manner.
Authors: Roest Et al.
Cells 2018;7
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When PERK inhibitors turn out to be new potent RIPK1 inhibitors: critical issues on the specificity and use of GSK2606414 and GSK2656157.
Authors: Rojas-Rivera Et al.
Cell Death Differ 2017;24:1100
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