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 |
