In Vitro: 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.
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.