FKBP12 PROTAC RC32

FKBP12 PROTAC RC32 (RC32) is a potent FKBP12 degrader based on PROTAC technology. FKBP12 PROTAC RC32 contains conjugation of Rapamycin ( HY-10219 ) and a ligand for an Cereblon E3 ubiquitin ligase (Pomalidomide; HY-10984) In Vitro FKBP12 PROTAC RC32 (RC32; 0.1-1000 nM; for 12 hours) results in 50% protein degradation (DC 50 ) of ~0.3 nM after only 12 hours of treatment. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: Jurkat cells Concentration: 0.1, 1, 10, 100, 1000 nM Incubation Time: For 12 hours Result: Resulted in 50% protein degradation (DC 50 ) of ~0.3 nM after only 12 h of treatment. In Vivo 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 . RC32 (orally; 60 mg/kg; twice a day; for 1 day) significantly degrades FKBP12 in mice . 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) . 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male and female mice Dosage: 30 mg/kg Administration: IP; twice a day; 1 day Result: Degraded the FKBP12 protein in most of the organs of treated mice after only 1 day of treatment. Form:Solid IC50& Target:Cereblon

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