APY29 --- IRE1a Modulator

Bioss

APY29 --- IRE1a Modulator [1216665-49-4]

16

Research Use Only

98.0

APY29 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, APY29 occupies IRE1alphas kinase ATP-binding site to activate RNase-mediated XBP1 mRNA splicing even without upstream endoplasmic reticulum stress. It dose-dependently reduces IRE1alpha kinase autophosphorylation in vitro with IC50 ~0.28 microM. As dysregulation of the UPR has been implicated in a variety of cell degenerative and neoplastic disorders, small molecule modulators of IRE1alpha, such as APY29, serve as useful tools to understand the UPRs role in pathophysiology and to develop drugs for endoplasmic reticulum stress-related diseases.

-20°C

51202000