CCT367766

CCT367766 is a pirin PROTAC degrader. CCT367766 forms a ternary complex with cereblon and induces pirin depletion via the ubiquitin-proteasome pathway in a concentration- and time-dependent manner. CCT367766 can be used for ovarian cancer research^[1][2][3]. IC50 & Target:IC50: 490 nM (CRBN-DDB1 complex); Kd: 55 nM (pirin), 120nM (CRBN)^[1] In Vitro:CCT367766 (0.5 nM; 2 hr) potently and selectively induces cereblon- and proteasome-dependent degradation of pirin in SKOV3 human ovarian cancer cells, with detectable depletion at 0.5 nM after 2 hours of treatment, and causes a 2.3-fold reduction in pirin abundance with no significant effects on other quantifiable proteins in the proteome^[3].
CCT367766 (0.5-1500 nM; 2-24 h) potently and selectively depletes pirin in SK-OV-3 human ovarian carcinoma cells, with near-complete degradation observed at 50 nM for 2 h, and intracellular target engagement confirmed via competition with pirin-binding ligands^[1].
CCT367766 binds recombinant pirin with high affinity (K_d = 55 nM) and recombinant CRBN-DDB1 complex with moderate affinity (K_i = 120 nM), while possessing physicochemical properties including a LogD_7.4 of 2.7 and kinetic solubility of 2 μM^[1].
CCT367766 (50 nM; 2 h) potently and selectively degrades pirin in cancer cells, achieving nearly complete degradation at 50 nM after 2 h of incubation^[2].