生物活性 | |||
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描述 | PROTAC BET degrader-9 is PROTAC targeting on BET proteins, consist of a BET inhibitor HJB97 as the warhead ligand and Pomalidomide as CRBN ligand. PROTAC BET degrader-9 at concentration of 3, 10 and 30nM led a dose-dependent degradation of BRD2, 3 and 4 at different levels post 3-hour treatment in RS4;11 cells. PROTAC BET degrader-25 exhibited potency against MOLM-13 and RS4;11 with IC50 values of 4.3nM and 45.5nM, respectively[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.15mL 0.23mL 0.11mL |
5.73mL 1.15mL 0.57mL |
11.47mL 2.29mL 1.15mL |
参考文献 |
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