产品简介:
APY29 是一种I类IRE1α抑制剂,与IRE1α的ATP结合位点相结合,抑制其自我磷酸化(IC50 = 280 nM)、增强其RNase作用(EC50 = 460 nM)。
分子式:C17H16N8 分子量:332.36
物理性状及指标:
外观:……………………粉末
溶解性:…………………32 mg/mL (96.28 mM);H2O:Insoluble
含量:……………………>98%
储存条件:
-20℃,避光防潮密闭干燥
运输条件:
2~8℃运输
描述 | APY29, an ATP-competitive inhibitor, is an allosteric modulator ofIRE1αwhich inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket withIC50of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain. |
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IC50& Target | IC50: 280 nM (IRE1α) |
体外研究 | 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. |
按表中溶解性配置;如溶解困难,可以通过快速搅拌,超声或温和加热(在45-60°C下水浴)。液体稳定性报道的很少,建议现配现用,如需储存,建议:-20℃ 1-3月;-80℃ 3-6月。 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.0088 mL | 15.0439 mL | 30.0879 mL |
5 mM | 0.6018 mL | 3.0088 mL | 6.0176 mL |
10 mM | 0.3009 mL | 1.5044 mL | 3.0088 mL |
50 mM | 0.0602 mL | 0.3009 mL | 0.6018 mL |
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