AMG PERK 44
SIGMA/SML3049 - ≥98% (HPLC)
Synonym: 4-
CAS Number: 1644664-21-0 (free base)
Empirical Formula (Hill Notation): C34H28N4O2 · xHCl
Molecular Weight: 524.61 (free base basis)
Linear Formula: C34H28N4O2 · xHCl
Product Type: Chemical
assay | ≥98% (HPLC) |
color | white to beige |
form | powder |
Quality Level | 100 ![]() |
SMILES string | O=C1N(N(C(C2=CC=CC=C2)=C1 |
solubility | DMSO: 2 mg/mL, clear |
storage temp. | −20°C |
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 μM, b-Raf IC50 >1 μM, <65% inhibition at 1 μM 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/kg & ED90 = 60 mg/kg 4 hr post po.). |
Purity | ≥98% (HPLC) |
Storage Temp. | −20°C |
UNSPSC | 12352200 |