ZLD1039

Description: ZLD1039 is a potent, orally bioavailable EZH2 (Enhancer of Zeste Homolog 2) inhibitor with high selectivity. It demonstrates strong, concentration-dependent inhibition of both wild-type and mutant (Y641F and A677G) PRC2 (Polycomb Repressive Complex 2) enzymatic activities, exhibiting IC50 values of 5.6, 15, and 4.0 nM, respectively. Additionally, ZLD1039 effectively suppresses breast tumor growth and metastasis. Target: Histone Methyltransferase. Smiles: CCN(C1CCOCC1)c1cc(cc(C(=O)NCc2c3CCCCc3c(C)[nH]c2=O)c1C)-c1ccc(nc1)N1CCN(C)CC1. References: Xuejiao Song, et al. Selective inhibition of EZH2 by ZLD1039 blocks H3K27methylation and leads to potent anti-tumor activity in breast cancer. Sci Rep. 2016, 6: 20864.