APY29

产品名称：

1216665-49-4
APY29
N2-1H-Benzimidazol-6-yl-N4-(5-cyclopropyl-1H-pyrazol-3-yl)-2,4-pyrimidinediamine
APY29 (type I kinase inhibitor)
N2-(1H-Benzo[d]imidazol-6-yl)-N4-(3-cyclopropyl-1H-pyrazol-5-yl)pyrimidine-2,4-diamine
APY 29
APY-29

产品介绍：

产品说明

一般描述

APY29 is considered as a type I kinase inhibitor of inositol requiring kinase enzyme 1 α (IRE1α).

生化/生理作用

APY29 is a small molecule that inhibits the kinase activity of IRE1α (in vitro autophosphorylation IC50 = 280 nM) by targeting its active site ATP-binding pocket, while simultaneously acting as an allosteric activator of IRE1α RNase activity (EC50 = 460 nM) by keeping the active site in an open conformation. When applied 1 hr prior to stress induction by 4-hr 6 nM thapsigargin treatment, APY29 significantly potentiates stress-induced unfolded protein response (UPR) in rat insulinoma INS-1 cultures (XBP1 mRNA processing induction = 54% without vs. 78% with 1-hr 3 μM APY29 pretreatment).
APY29 has the ability to enhance inositol requiring kinase enzyme 1 α (IRE1α) (P830L)′s oligomeric state to rescue RNase activity.

基本信息

经验(实验)分子式	C₁₇H₁₆N₈
分子量	332.36
MDL编号	MFCD27991280

产品性质

测定	≥97% (HPLC)
形式	powder
颜色	white to beige
溶解性	DMSO: 2 mg/mL, clear
储存温度	−20℃
SMILES string	C1(NC2=CC(C3CC3)=NN2)=CC=NC(NC4=CC=C(N=CN5)C5=C4)=N1

安全信息

储存分类代码	13 - Non Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable