tcsc2552 APY29

APY29 is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation with IC₅₀ of 280 nM and activates IRE1α RNase activity.

IC50 & Target: IC50: 280 nM (IRE1α)

In Vitro: APY29 divergently modulates the RNase activity and oligomerization state of IRE1α. APY29 is exerting their opposing effects on RNase activity through the same binding site. APY29 divergently affects IRE1α oligomerization. APY29 demonstrates opposing dose-dependent effects on ER stress-induced activation of the RNase of endogenous IRE1α^[1].