APY29
Synonyms:
N2-(1H-Benzo[d]imidazol-6-yl)-N4-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine
APY29 is a highly potent and selective allosteric modulator of IRE1α. Under endoplasmic reticulum (ER) stress, unfolded proteins accumulate in the ER to activate the ER transmembrane kinase/endoribonuclease (RNase)—IRE1α
IRE1α oligomerizes, autophosphorylates, and initiates splicing of XBP1 mRNA, thus triggering the unfolded protein response (UPR). APY29 Inhibits IRE1α autophosphorylation (IC₅₀ = 280 nM) and activates IRE1αRNase activity. As dysregulation of the UPR has been implicated in a variety of cell degenerative and neoplastic disorders, small molecule modulators of IRE1α should be very useful in understanding UPR’s role in pathophysiology and to develop drugs for ER stress-related diseases.
Formula:
C₁₇H₁₆N₈ MW: 332,36 g/mol |
MDL Number:
MFCD28023582 CAS Number: 1216665-49-4 |
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