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General description
APY29 is considered as a type I kinase inhibitor of inositol requiring kinase enzyme 1 α (IRE1α).
Biochem/physiol Actions
APY29 has the ability to enhance inositol requiring kinase enzyme 1 α (IRE1α) (P830L)′s oligomeric state to rescue RNase activity.
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).
ATP-competitive IRE1α kinase activity inhibitor and allosteric IRE1α RNase activity activator that enhances stress-induced unfolded protein response (UPR).
| assay | ≥97% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | −20°C |
| SMILES string | C1(NC2=CC(C3CC3)=NN2)=CC=NC(NC4=CC=C(N=CN5)C5=C4)=N1 |
| InChI | 1S/C17H16N8/c1-2-10(1)13-8-16(25-24-13)22-15-5-6-18-17(23-15)21-11-3-4-12-14(7-11)20-9-19-12/h3-10H,1-2H2,(H,19,20)(H3,18,21,22,23,24,25) |
| InChI key | WJNBSTLIALIIEW-UHFFFAOYSA-N |
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¥ 2707.32
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¥ 1683.78
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¥ 1259.40
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¥ 5167.58
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¥ 2883.61
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¥ 3852.13
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¥ 1196.14
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