生物活性 | |||
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描述 | PROTAC BET degrader-25 is PROTAC targeting on BET proteins, consist of a BET inhibitor HJB97 as the warhead ligand and a Lenalidomide analogue as the CRBN ligand. PROTAC BET degrader-25 at concentration of 10, 30 and 100nM 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 9.6nM and 72.3nM, respectively[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.30mL 0.26mL 0.13mL |
6.49mL 1.30mL 0.65mL |
12.97mL 2.59mL 1.30mL |
参考文献 |
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