1216665-49-4

1216665-49-4 structure

Name: APY 29
Chemical Name: apy29
CAS Number: 1216665-49-4
Molecular Formula: C₁₇H₁₆N₈
Molecular Weight: 332.362
Catalog: Signaling Pathways Cell Cycle/DNA Damage IRE1
Create Date: 2017-04-17 11:41:24
Modify Date: 2024-01-08 18:52:12
APY29 is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation with IC50 of 280 nM and activates IRE1α RNase activity.

Name	apy29
Synonyms	2,4-Pyrimidinediamine, N-1H-benzimidazol-5-yl-N-(3-cyclopropyl-1H-pyrazol-5-yl)- N2-1H-Benzimidazol-6-yl-N4-(5-cyclopropyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine N-(1H-Benzimidazol-5-yl)-N-(3-cyclopropyl-1H-pyrazol-5-yl)-2,4-pyrimidinediamine

Description	APY29 is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation with IC50 of 280 nM and activates IRE1α RNase activity.
Related Catalog	Signaling Pathways >> Cell Cycle/DNA Damage >> IRE1 Research Areas >> Cancer
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].
References	[1]. Wang L, et al. Divergent allosteric control of the IRE1α endoribonuclease using kinase inhibitors. Nat Chem Biol. 2012 Dec;8(12):982-9.