FKBP12PROTACRC32(RC32)是基于PROTAC的有效FKBP12降解剂。FKBP12PROTACRC32包含雷帕霉素(Rapamycin)和E3泛素连接酶配体(Pomalidomide)。
FKBP12 PROTAC RC32 (RC32) is a potent FKBP12 degrader based on PROTAC technology. FKBP12 PROTAC RC32 contains conjugation of Rapamycin and a ligand for an E3 ubiquitin ligase (Pomalidomide)[1].
FKBP12 PROTAC RC32 (RC32; 0.1-1000 nM; for 12 hours) results in 50% protein degradation (DC50) of ~0.3 nM after only 12 hours of treatment[1]. Western Blot Analysis[1] Cell Line: Jurkat cells
RC32 (RC32; i.p.; 30 mg/kg; twice a day; 1 day) degrades the FKBP12 protein in most of the organs of treated mice, except for the brain after only 1 day of treatment in mice[1]. RC32 (orally; 60 mg/kg; twice a day; for 1 day) significantly degrades FKBP12 in mice[1]. RC32 (i.p.; 8 mg/kg; twice a day; for 2 days) efficiently degrades the FKBP12 protein in most of the organs examined in Bama pigs (20 kg) [1]. RC32 (i.p.; 8 mg/kg; twice a day; for 3 days) efficiently degrades FKBP12 in the heart, liver, kidney, spleen, lung, and stomach of rhesus monkeys[1]. Animal Model: Male and female mice[1]
[1]. A chemical approach for global protein knockdown from mice to non-human primates. Cell Discov. 2019 Feb 5;5:10.
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