Chemren Bio-Engineering Co., Ltd.

Biological Activity of APY29

 

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.

Divergent allosteric control of the IRE1α endoribonuclease using kinase inhibitors
By Wang, Likun; Perera, B. Gayani K.; Hari, Sanjay B.; Bhhatarai, Barun; Backes, Bradley J.; Seeliger, Markus A.; Schuerer, Stephan C.; Oakes, Scott A.; Papa, Feroz R.; Maly, Dustin J.
From Nature Chemical Biology (2012), 8(12), 982-989. 

 

References on APY29

[1]. Wang L, et al. Divergent allosteric control of the IRE1α endoribonuclease using kinase inhibitors. Nat Chem Biol. 2012 Dec;8(12):982-9.

[2]. Korennykh AV, et al. The unfolded protein response signals through high-order assembly of Ire1. (2009) Nature. 457(7230):687-93.

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Chemical Information

M.Wt	332.36	Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Formula	C17H16N8
CAS No	1216665-49-4
Solubility	DMSO

 

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