NUCC-0226272, a potent PROTAC, induces the degradation of EZH2 and exhibits anti-proliferative effects. It holds promise for application in cancer research [1].

NUCC-0226272 exhibits antiproliferative effects on LNCaP and 22Rv1 cells at concentrations of 0.01-10 μM over 5 days. At 10 μM over 6 days, it shows significant degradation of EZH2, reduction of the PRC2 component SUZ12, and decreased levels of H3K27me3 in C4-2B cells [1].

Pharmacokinetic parameters of NUCC-0226272 in C57Bl/6 mice [1] are as follows: after an IP dose of 4 mg/kg, T_max is 0.83 hours, C_max reaches 3650 ng/mL, AUC_last is 12777389 min·ng/mL, t_1/2 is 3.46 hours, clearance (CL) is 3.11 mL/min/kg, and volume of steady-state distribution (V_ss) is 3.11 L/kg.