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生物活性
In the absence of proteasomes, Usp14 is insensitive to IU1, suggesting that IU1 binds specifically to the activated form of Usp14. IU1 could potentially inhibit Usp14 by preventing its docking on the proteasome. IU1 could enhance proteasome function in cells to accelerates proteolysis. Moreover, IU1 inhibits chain trimming and stimulates substrate degradation in vitro which could potentially have therapeutic applications for diseases involving toxic proteins that are proteasome substrates.
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体外研究
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体内研究
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激酶实验
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细胞实验
~1.5 mM
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动物实验
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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）
|  动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 |
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例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。
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参考文献
[1] Byung-Hoon L, et al. Nature, 2010, 467(7312), 179-184.
[2] Lee et al (2010) Enhancement of proteasome activity by a small-molecule inhibitor of USP14. Nature 467 179.
[3] Lee et al (2010) Trimming of ubiquitin chains by proteasome-associated deubiquitinating enzymes. Mol.Cell.Proteomics 10 R110.
分子式
C18H21FN2O |
分子量
300.37 |
CAS号
314245-33-5 |
储存方式
﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂（常温）
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DMSO
60 mg/mL |
Water
<1 mg/mL |
Ethanol
60 mg/mL |
体内溶解度
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Clinical Trial Information ( data from http://clinicaltrials.gov )
注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。
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