For research use only. Not for therapeutic Use.
APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain[1].
APY29 divergently modulates the RNase activity and oligomerization state of IRE1α. APY29 is exerting their opposing effects on RNase activity through the same binding site. APY29 divergently affects IRE1α oligomerization. APY29 demonstrates opposing dose-dependent effects on ER stress-induced activation of the RNase of endogenous IRE1α[1].
| Catalog Number | I000817 |
| CAS Number | 1216665-49-4 |
| Synonyms | 2-N-(3H-benzimidazol-5-yl)-4-N-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine |
| Molecular Formula | C17H16N8 |
| Purity | ≥95% |
| InChI | 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) |
| InChIKey | WJNBSTLIALIIEW-UHFFFAOYSA-N |
| SMILES | C1CC1C2=CC(=NN2)NC3=NC(=NC=C3)NC4=CC5=C(C=C4)N=CN5 |
| Reference | [1]. Wang L, et al. Divergent allosteric control of the IRE1α endoribonuclease using kinase inhibitors. Nat Chem Biol. 2012 Dec;8(12):982-9. |
