APY29

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Chemical Structure| 1216665-49-4 同义名 : -
CAS号 : 1216665-49-4
货号 : A724754
分子式 : C17H16N8
纯度 : 99%+
分子量 : 332.363
MDL号 : MFCD28023582
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(150.44 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 5 mg/mL(15.04 mM)，配合低频超声，并调节pH至3
动物实验配方：
生物活性
描述 IRE1 (inositol requiring enzyme 1) is an ER transmembrane sensor that activates UPR to maintain ER and cellular function. It can promotes cell survive and initiate apoptosis via decay of anti-apoptotic microRNAs[2]. APY29 is a modulator of IRE1α by binding to the ATP-binding site and inhibits it autophosphorylation (IC50=280nM) and enhances its RNase function (EC50=460nM). In vitro, it restores the ability of dephosphoylated IRE1α to cleave XBP1 mRNA in a dose-dependent manner. It also enhances IRE1α oligomerization in a crosslinking assay[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.01mL

0.60mL

0.30mL

15.04mL

3.01mL

1.50mL

30.09mL

6.02mL

3.01mL
参考文献

[1]Wang L, Perera BG, et al. Divergent allosteric control of the IRE1α endoribonuclease using kinase inhibitors. Nat Chem Biol. 2012 Dec;8(12):982-9.

[2]Chen Y, Brandizzi F. IRE1: ER stress sensor and cell fate executor. Trends Cell Biol. 2013 Nov;23(11):547-55.

[3]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.