APY29

APY29

Biochem/physiol Actions

APY29 is a small molecule that 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 rat insulinoma INS-1 cultures (XBP1 mRNA processing induction = 54% without vs. 78% with 1-hr 3 µM APY29 pretreatment).

APY29 has the ability to enhance inositol requiring kinase enzyme 1 ? (IRE1?) (P830L)?s oligomeric state to rescue RNase activity.

General description

APY29 is considered as a type I kinase inhibitor of inositol requiring kinase enzyme 1 ? (IRE1?).

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Code Description Colour Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3576234 APY29 white to beige SIGMA-ALDRICH −20°C DMSO: 2 mg/mL, clear powder ≥97% (HPLC)
£339.86 (exc VAT) per 25MG
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3576235 APY29 white to beige SIGMA-ALDRICH −20°C DMSO: 2 mg/mL, clear powder ≥97% (HPLC)
£84.41 (exc VAT) per 5MG
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