APY29 --- IRE1a Modulator

Overview
Catalog #	bs-60168c-2-mg-solid
Product Name	APY29 --- IRE1a Modulator
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 332.36 Formula: C17 H16 N8 CAS Number: 1216665-49-4 InChi Key: WJNBSTLIALIIEW-UHFFFAOYSA-N 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) Smiles: C1CC1C1=CC(NC2C=CN=C(NC3=CC4NC=NC=4C=C3)N=2)=NN1 Purity: 98.0 Solubility: DMSO up to 100 mM Appearance: Solid Power. Shelf Life: 1.0 years
Description	APY29 is a highly potent and selective small molecule modulator of IRE1α. Under endoplasmic reticulum stress, unfolded protein accumulation leads to activation of the endoplasmic reticulum transmembrane kinase/endoRNase (RNase) IRE1α. IRE1α oligomerizes, autophosphorylates and initiates splicing of XBP1 mRNA, thus triggering the unfolded protein response (UPR). Interestingly, APY29 occupies IRE1α's kinase ATP-binding site to activate RNase-mediated XBP1 mRNA splicing even without upstream endoplasmic reticulum stress. It dose-dependently reduces IRE1α kinase autophosphorylation in vitro with IC50 ~0.28 µM. As dysregulation of the UPR has been implicated in a variety of cell degenerative and neoplastic disorders, small molecule modulators of IRE1α, such as APY29, serve as useful tools to understand the UPR's role in pathophysiology and to develop drugs for endoplasmic reticulum stress-related diseases.