jq-ez-05-jqez5

Description: JQ-EZ-05 (also abbreviated as JQEZ5) is a novel, potent, specific and reversible inhibitor of EZH2 (overexpressed in tumor cells such as lung cancer). Epigenetic targets are exciting new avenues for the discovery of targeted anticancer drugs. Zhang etc. have designed the open-source EZH2 inhibitor JQEZ5 which showed potent antitumor efficacy in vitro and in vivo in preclinical studies in murine and human lung adenocarcinoma models expressing high levels of EZH2. EZH2 is a lysine methyltransferase and acts as master regulator of chromatin function, it orchestrates transcriptional silencing of developmental gene networks. Overexpression of EZH2 is commonly observed in human epithelial cancers, such as non-small cell lung carcinoma (NSCLC), yet definitive demonstration of malignant transformation by deregulated EZH2 remains elusive.

References: Cancer Discov. 2016 Sep; 6(9):1006-21; Cancer Discov. 2016 Sep; 6(9):949-52; WO2015148716A1.