IRE-3 --- IRE1a Modulator

Overview
Catalog #	bs-60167c-2mg-solid
Product Name	IRE-3 --- IRE1a Modulator
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 504.51 Formula: C27 H23 F3 N6 O CAS Number: 1414938-21-8 InChi Key: MEJKZYOOTMLMBA-UHFFFAOYSA-N InChi: InChI=1S/C27H23F3N6O/c1-15(2)25-35-22(23-24(31)32-12-13-36(23)25)20-10-11-21(19-9-4-3-8-18(19)20)34-26(37)33-17-7-5-6-16(14-17)27(28,29)30/h3-15H,1-2H3,(H2,31,32)(H2,33,34,37) Smiles: CC(C)C1=NC(=C2C(N)=NC=CN21)C1=CC=C(NC(=O)NC2=CC(=CC=C2)C(F)(F)F)C2=CC=CC=C21 Purity: 98.0 Solubility: DMSO up to 50 mM Appearance: Solid Power. Shelf Life: 1.0 years
Description	IRE-3 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, IRE-3 inhibits the XBP1 mRNA splicing through binding to the IRE1α ATP-binding site, even under endoplasmic reticulum stress. It shows dose-dependent reduction of IRE1α kinase autophosphorylation in vitro with IC50~3.12 µM. IRE-3 can also block enzymatic activities of IRE1α in INS-1 rat insulinoma cell lines. As dysregulation of the UPR has been implicated in a variety of cell degenerative and neoplastic disorders, small molecule modulators of IRE1α, such as IRE-3 and APY-29, serve as useful tools to understand the UPR's role in pathophysiology and to develop drugs for endoplasmic reticulum stress-related diseases.