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IU1

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Chemical Structure| 314245-33-5 同义名 : -
CAS号 : 314245-33-5
货号 : A875547
分子式 : C18H21FN2O
纯度 : 98%
分子量 : 300.371
MDL号 : MFCD01917473
存储条件:

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 40 mg/mL(133.17 mM),配合低频超声助溶,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

动物实验配方:
生物活性
靶点
  • USP/UBP

    USP14, IC50:4.7 μM

描述 Usp14, a proteasome-associated deubiquitinating enzyme, can impede the degradation of ubiquitin-protein conjugates, both in vivo and in vitro. IU1 inhibits the catalytic activity of proteasome-associated Usp14 in vitro, with an IC50 of 4-5 μM. IU1 specifically binds to the activated form of Usp14 and may inhibit it by preventing its docking on the proteasome. However, direct tests of this scenario yielded negative results. Usp14 inhibition is rapidly established upon IU1 addition and rapidly reversed upon its removal. IU1 also promotes the degradation of Sic1, a CDK inhibitor from S. cerevisiae [1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.33mL

0.67mL

0.33mL

16.65mL

3.33mL

1.66mL

33.29mL

6.66mL

3.33mL

参考文献

[1]Lee BH, et al. Enhancement of proteasome activity by a small-molecule inhibitor of USP14. Nature. 2010 Sep 9;467(7312):179-84.