生物活性
APY29 inhibits IRE1α autophosphorylation (IC50 = 280 nM) and activates IRE1α ribonuclease activity. APY29 occupies IRE1α's kinase ATP-binding site to activate RNase-mediated XBP1 mRNA splicing even without upstream endoplasmic reticulum stress. It dose-dependently reduces IRE1α kinase autophosphorylation in vitro with IC50 ~0.28 μM. As dysregulation of the UPR has been implicated in a variety of cell degenerative and neoplastic disorders, small molecule modulators of IRE1α, such as APY29, serve as useful tools to understand the UPR's role in pathophysiology and to develop drugs for endoplasmic reticulum stress-related diseases.
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| | 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量，需要将22.4 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。
化学数据
| 分子量 | 332.36 |
| 分子式 | C17H16N8 |
| CAS号 | 1216665-49-4 |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO |
| 储存和运输条件 | -20°C 冷藏长期储存
常温运输及临时存放 |
参考文献
Divergent allosteric control of the IRE1α endoribonuclease using kinase inhibitors.
Wang L, et al. Nat Chem Biol. 2012 Dec;8(12):982-9. PMID: 23086298.
The unfolded protein response signals through high-order assembly of Ire1.
Korennykh AV, et al. Nature. 2009 Feb 5;457(7230):687-93. PMID: 19079236.
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