Synonyms: 4-(2-Amino-4-methyl-3-(2-methylquinolin-6-yl)benzoyl)-1-methyl-2,5-diphenyl-1H-pyrazol-3(2H)-one hydrochloride; 4-[2-Amino-4-methyl-3-(2-methyl-6-quinolinyl)benzoyl]-1,2-dihydro-1-methyl-2,5-diphenyl-3H-pyrazol-3-one hydrochloride; AMG'44; AMG44; Compound 44; PERK inhibitor 44; PERK-IN-1
Molecular Formula: C34H28N4O2 · xHCl
Linear Structural Formula: C34H28N4O2 · xHCl
Purity: >=98% (HPLC)
Storage: -20C
Biochem Physiol Actions: AMG PERK 44 (AMG44) is an orally active (F = 46% (mouse) & 55% (rat) post 2.5 mg/kg po.), active site-targeing, potent and highly selective PERK (EIF2AK3) inhibitor (IC50 = 6 nM; GCN2 IC50 = 7.3 muM, b-Raf IC50 >1 muM,<65 % inhibition at 1 mum against 387 kinases). amg44 inhibits cellular perk autophosphorylation (pt980 ic50="84" nm; ht1080 t-rex-perk-flag transfectants) and er stress-induced bulk protein synthesis (ic50="400" nm; u2os), as well as perk pt980 in ht1080 matrigel plug implant in mice in vivo (ed50="3" mg g & ed90="60" mg g 4 hr post po.).<>