APY29

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

APY29 是 IRE1α 的变构调节剂；抑制 IRE1α 自磷酸化 (IC50 = 280 nM) 并激活 IRE1α RNase 活性。

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.

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.

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APY29 | APY-29 | APY 29

Neuroscience

P2 Receptor

IRE1α

Cancer

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1216665-49-4

332.36

C17H16N8

>98% (HPLC)

DMSO : 10 mg/mL. 30.09 mM;

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

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

(-20℃)

With Ice Pack

≥ 2 years