IRE-3 --- IRE1a Modulator

Bioss

IRE-3 --- IRE1a Modulator [1414938-21-8]

16

Research Use Only

98.0

IRE-3 is a highly potent and selective small molecule modulator of IRE1alpha. Under endoplasmic reticulum stress, unfolded protein accumulation leads to activation of the endoplasmic reticulum transmembrane kinase/endoRNase (RNase) IRE1alpha. IRE1alpha 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 IRE1alpha ATP-binding site, even under endoplasmic reticulum stress. It shows dose-dependent reduction of IRE1alpha kinase autophosphorylation in vitro with IC50~3.12 microM. IRE-3 can also block enzymatic activities of IRE1alpha 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 IRE1alpha, such as IRE-3 and APY-29, serve as useful tools to understand the UPRs role in pathophysiology and to develop drugs for endoplasmic reticulum stress-related diseases.

-20°C

51202000