APY29( APY29 | APY-29 | APY 29 )

Catalog No. M17198 CAS No. 1216665-49-4

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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Product Name

APY29
Note

Research use only, not for human use.
Brief Description

APY29 is an allosteric modulator of IRE1α; inhibits IRE1α autophosphorylation (IC50 = 280 nM) and activates IRE1α RNase activity.
Description

APY29 is a IRE1α inhibitor. The accumulation of unfolded proteins under endoplasmic reticulum (ER) stress leads to the activation of the multidomain protein sensor IRE1α as part of the unfolded protein response (UPR). ATP-competitive inhibitors of IRE1α promote dimerization and activation of RNase activity despite blocking kinase autophosphorylation.
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.
In Vivo

——
Synonyms

APY29 | APY-29 | APY 29
Pathway

Neuroscience
Target

P2 Receptor
Recptor

IRE1α
Research Area

Cancer
Indication

——

CAS Number

1216665-49-4
Formula Weight

332.36
Molecular Formula

C17H16N8
Purity

>98% (HPLC)
Solubility

DMSO : 10 mg/mL. 30.09 mM;
SMILES

C1CC1c1cc(n[nH]1)Nc1nc(ncc1)Nc1cc2c(cc1)nc[nH]2
Chemical Name

(E)-N-(6-((5-cyclopropyl-1H-pyrazol-3-yl)imino)-1,6-dihydropyrimidin-2-yl)-1H-benzo[d]imidazol-6-amine

1. Wang L, et al. Nat Chem Biol. 2012 Dec;8(12):982-9.

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