CCT367766

CCT367766 is a potent and the third generation heterobifunctional and Cereblon-based pirin targeting protein degradation probe (PDP, or PROTAC), depletes pirin protein expression at low concentration. CCT367766 exhibits a moderate affinity for the CRBN-DDB1 complex with an IC₅₀ value of 490 nM. CCT367766 reveals a good affinity for the recombinant pirin and CRBN with K_d values of 55 nM and 120 nM, respectively. CCT367766 provides a potential chemical tool to study a largely unexplored protein^[1]. IC50 & Target:IC50: 490 nM (CRBN-DDB1 complex); Kd: 55 nM (pirin), 120nM (CRBN)^[1] In Vitro: CCT367766 (50-1500 nM; 24 hours) demonstates the depletion of pirin protein as a the time-dependent hook-effect in SK-OV-3 human ovarian cancer cells^[1].
CCT367766 (0.5-50 nM; 2 hours) demonstrates the concentration-dependent depletion of pirin protein after 2 h exposure in SK-OV-3 cells^[1].
CCT367766 (0.5-50 nM; 2 hours) dose-dependently rescuses pirin expression from pretreatment of chlorobisamide in SK-OV-3 cells^[1].