A modulator of IRE1α function
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APY-29

Item No. 22913

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N2-1H-benzimidazol-6-yl-N4-(5-cyclopropyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine
CAS Number
1216665-49-4
Molecular Formula
C17H16N8
Formula Weight
332.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlEthanol: 15 mg/mlEthanol:PBS (pH 7.2) (1:3): 0.25 mg/ml
λmax
249, 273, 306 nm
SMILES
C1(NC2=NNC(C3CC3)=C2)=CC=NC(NC4=CC=C(N=CN5)C5=C4)=N1
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    Product Description

    APY-29 is a modulator of inositol requiring enzyme 1 α (IRE1α), which is a protein located in the endoplasmic reticulum (ER) membrane that has kinase and RNase activities triggered by ER stress.1 It binds to the ATP-binding site on IRE1α, where it inhibits its autophosphorylation (IC50 = 280 nM) and enhances its RNase function (EC50 = 460 nM). In vitro, it restores the ability of dephosphoylated IRE1α to cleave XBP1 mRNA in a dose-dependent manner. It also enhances IRE1α oligomerization in a crosslinking assay.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, L., Perera, B.G., Hari, S.B., et al. Divergent allosteric control of the IRE1α endoribonuclease using kinase inhibitors. Nat. Chem. Biol. 8(12), 982-989 (2012).