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APY29
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
APY29图片
CAS NO:1216665-49-4
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
25mg电议
50mg电议

产品介绍
APY29 是一种 ATP 竞争性抑制剂，是 IRE1α 的变构调节剂，通过与 ATP 结合口袋结合来抑制 IRE1α 自磷酸化，IC50 为 280 nM。 APY29 作为配体，变构激活 IRE1α 相邻的 RNase 结构域。
Cas No.1216665-49-4
化学名(E)-N-(6-((5-cyclopropyl-1H-pyrazol-3-yl)imino)-1,6-dihydropyrimidin-2-yl)-1H-benzo[d]imidazol-6-amine
Canonical SMILESC1(C2=CC(/N=C(N3)\C=CN=C3NC4=CC5=C(N=CN5)C=C4)=NN2)CC1
分子式C17H16N8
分子量332.36
溶解度≥ 16mg/mL in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

APY29 is an inhibitor of IRE1α with IC50 value of 0.28μM [1].

IRE1α is a transmembrane protein in ER. It can be activated when unfolded proteins accumulate in ER. APY29 is found to interact with the ATP-binding site of wild-type IRE1α and activate the kinase activity of IRE1α even without upstream ER stress. APY29 acts as a slight activator and stabilizes IRE1α’s kinase domain in an alternative conformation. It is found to restore the ability of dephosphorylated IRE1α to cleave the substrate XBP1 up to about 60% of the levels of normal IRE1α. Furthermore, APY29 increases the oligomer/monomer ratio of IRE1α and finally displays a decrease of IRE1α trans-autophosphorylation [1].

References:
[1] Wang L, Perera BG, Hari SB, Bhhatarai B, Backes BJ, Seeliger MA, Schürer SC, Oakes SA, Papa FR, Maly DJ. Divergent allosteric control of the IRE1α endoribonuclease using kinase inhibitors. Nat Chem Biol. 2012 Dec;8(12):982-9.