APY29 is considered as a type I kinase inhibitor of inositol requiring kinase enzyme 1 a (IRE1a).
Synonyms: APY 29; APY-29; APY29 (type I kinase inhibitor); N2-(1H-Benzo[d]imidazol-6-yl)-N4-(3-cyclopropyl-1H-pyrazol-5-yl)pyrimidine-2,4-diamine; N2-1H-Benzimidazol-6-yl-N4-(5-cyclopropyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine
Molecular Formula: C17H16N8
Molecular Weight: 332.36
Linear Structural Formula: C17H16N8
MDL Number: MFCD27991280
Purity: >=97% (HPLC)
Storage: -20C
Biochem Physiol Actions: APY29 is a small molecule that inhibits the kinase activity of IRE1alpha (in vitro autophosphorylation IC50 = 280 nM) by targeting its active site ATP-binding pocket, while simultaneously acting as an allosteric activator of IRE1alpha RNase activity (EC50 = 460 nM) by keeping the active site in an open conformation. When applied 1 hr prior to stress induction by 4-hr 6 nM thapsigargin treatment, APY29 significantly potentiates stress-induced unfolded protein response (UPR) in rat insulinoma INS-1 cultures (XBP1 mRNA processing induction = 54% without vs. 78% with 1-hr 3 muM APY29 pretreatment).