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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.
By permission of the authors
AMG PERK 44 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 561.07. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.2 mM||8.91 mL||44.56 mL||89.12 mL|
|1 mM||1.78 mL||8.91 mL||17.82 mL|
|2 mM||0.89 mL||4.46 mL||8.91 mL|
|10 mM||0.18 mL||0.89 mL||1.78 mL|
References are publications that support the biological activity of the product.
Smith et al (2015) Discovery of 1H-pyrazol-3(2H)-ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK). J.Med.Chem. 58 1426 PMID: 25587754
If you know of a relevant reference for AMG PERK 44, please let us know.
Keywords: AMG PERK 44, AMG PERK 44 supplier, AMGPERK44, PERK, inhibitors, inhibits, potent, selective, protein, kinase, R-like, PKR, ER, orally, bioavailable, 5517, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for AMG PERK 44 include:
Rojas-Rivera et al (2017) When PERK inhibitors turn out to be new potent RIPK1 inhibitors: critical issues on the specificity and use of GSK2606414 and GSK2656157. Cell Death Differ 24 1100 PMID: 28452996
Mahameed et al (2019) The unfolded protein response modulators GSK2606414 and KIRA6 are potent KIT inhibitors. Cell Death Dis 10 300 PMID: 30931942
Roest et al (2018) The ER Stress Inducer l-Azetidine-2-Carboxylic Acid Elevates the Levels of Phospho-eIF2α and of LC3-II in a Ca2+-Dependent Manner. Cells 7 PMID: 30513588
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