bix01294

BIX01294 is a **small molecule inhibitor** initially developed to target the **G9a histone methyltransferase (also known as EHMT2)**, specifically binding to its SET domain and inhibiting its methyltransferase activity[1][3][5][4][6]. By inhibiting G9a, BIX01294 reduces methylation of histone H3 lysine 9 (H3K9me2) and lysine 27 (H3K27me3), inducing cellular effects such as **autophagy, cell cycle arrest, and apoptosis** in multiple cancer cell lines including glioma, multiple myeloma, and diffuse large B-cell lymphoma[1][3][4][2][6]. BIX01294 also interferes with hypoxia-inducible factor-1 alpha (HIF-1α) stability and inhibits angiogenesis by blocking VEGF-induced signaling (VEGFR-2, FAK, paxillin pathways)[1]. It can additionally inhibit Jumonji histone demethylases, notably KDM3A, potentially contributing to EGFR signaling pathway inhibition in cancers such as non-small cell lung cancer[5]. BIX01294 is primarily used as an **experimental tool compound** for research on epigenetic modulation and is not an approved therapeutic agent for any indication. No brand name products are available.

Other names

bix-01294bix01294bix 01294