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)。
货号:ajcx30656
CAS:2375555-66-9
分子式:C75H107N7O20
分子量：1426.69
溶解度:DMSO: 10 mg/mL (7.01 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.