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AMG PERK 44

Chemical Structure : AMG PERK 44

CAS No.: 1883548-84-2

AMG PERK 44 (AMG44)

Catalog No.: PC-49287Not For Human Use, Lab Use Only.

AMG PERK 44 (AMG44) is a potent, highly selective, and orally active protein kinase RNA-like ER kinase (PERK) inhibitor with IC50 of 6 nM, inhibits cellular PERK autophosphorylation (pPERK) with IC50 of 84 nM.

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Biological Activity

AMG PERK 44 (AMG44) is a potent, highly selective, and orally active protein kinase RNA-like ER kinase (PERK) inhibitor with IC50 of 6 nM, inhibits cellular PERK autophosphorylation (pPERK) with IC50 of 84 nM.
AMG PERK 44 (AMG44) displays 1000-fold selectivity over GCN2, exquisite selectivity over a large panel of kinases.
AMG PERK 44 (AMG44) robustly inhibits PERK autophosphorylation (ED50=3 mg/kg; ED90=60 mg/kg) in a time course pharmacodynamic (PD) model assay.

Physicochemical Properties

M.Wt 561.08
Formula C34H29ClN4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-(2-Amino-4-methyl-3-(2-methylquinolin-6-yl)benzoyl)-1-methyl-2,5-diphenyl-1,2-dihydro-3H-pyrazol-3-one hydrochloride

References

1. Roest G, et al. Cells. 2018 Nov 30;7(12):239.

2. Diego Rojas-Rivera, et al. Cell Death Differ. 2017 Jun;24(6):1100-1110.

3. Smith AL,et al. J Med Chem 2015; 58: 1426–1441.

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