ZYZ384

ZYZ384 is a **novel small molecule inhibitor** developed as an anticancer agent. It specifically targets and inhibits **SMYD3** (SET and MYND domain-containing protein 3), a histone lysine methyltransferase implicated in cancer proliferation and epigenetic regulation. ZYZ384 impairs cancer cell growth in vitro and in vivo, most notably in **hepatocellular carcinoma**, by reducing H3K4 trimethylation at the Rac1 promoter, thereby triggering cell cycle arrest through the AKT pathway. ZYZ384 is also active in **non-small cell lung cancer** (NSCLC) with EGFR mutations, where it suppresses tumor growth by activating the **JNK/MAPK signaling pathway** and inducing apoptosis and cell cycle arrest in cancer cells resistant to EGFR inhibitors. In preclinical mouse models, ZYZ384 shows superior antitumor activity compared to sorafenib and exhibits low toxicity in normal tissues[1][2][3][4][7][9].