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JH-XI-10-02

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Chemical Structure| 2209085-22-1 同义名 : -
CAS号 : 2209085-22-1
货号 : A408682
分子式 : C53H69N5O9
纯度 : 99%
分子量 : 920.14
MDL号 : MFCD31813655
存储条件：

粉末

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(114.11 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
描述 JH-XI-10-02 is a PROTAC selectively targeting on CDK8 with IC50 value of 159nM, and is consist of a warhead target on CDK8 (a Cortistatin A derivate) linked to CRBN ligand Pomalidomide. JH-XI-10-02 at concentration of 1μM achieved an almost complete depletion of CDK8 in Jurkat cells post 24-hour treatment. The downregulation of its downstream, pSTAT1-S727, could also be observed[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.09mL

0.22mL

0.11mL

5.43mL

1.09mL

0.54mL

10.87mL

2.17mL

1.09mL
参考文献

[1]Hatcher JM, Wang ES, et al. Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8. ACS Med Chem Lett. 2018 Mar 18;9(6):540-545.