APY29

APY29 is a modulator of inositol requiring enzyme IRE1α, a protein sited in the endoplasmic recticulum that has kinase and RNase activities triggered by endoplasmic recticulum stress. It also functions in the allosteric control of IRE1α endoribonuclease using kinase inhibitors for the development of drugs for endoplasmic recticulum stress related diseases.

APY29 has the ability to enhance inositol requiring kinase enzyme 1 α (IRE1α) (P830L)μs oligomeric state to rescue RNase activity.', 'APY29 is a small molecule th at inhibits the kinase activity of IRE1α (in vitro autophosphorylation IC50 = 280 nM) by targeting its active site ATP-binding pocket, while simultaneously acting as an allosteric activator of IRE1α 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 r at insulinoma INS-1 cultures (XBP1 mRNA processing induction = 54% without vs. 78% with 1-hr 3 μM APY29 pretreatment).

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