APY29抑制剂、激动剂

规格 ：1216665-49-4

APY29抑制剂、激动剂（CAS号1216665-49-4）APY29是IRE1α变构调节剂，能抑制IRE1α自磷酸化，IC50为280 nM，能激活IRE1α RNase活性。 APY29 is an allosteric modulator of IRE1α; inhibits IRE1α autophosphorylation (IC50 = 280 nM) and activates IRE1α RNase activity.
IC50 value: 280 nM [1]
Target: IRE1α
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.