PBIT (2514-30-9) is a potent and selective inhibitor of JARID1 (IC50 = 3, 4.9 and 6 μM for JARID1B, 1A and 1C, respectively). The JARID1 (Jumonji AT-Rich Interactive Domain 1) family of lysine demethylases demethylates the trimethylated lysine 27 in histone H3 (H3K4me3). PBIT is selective for JARID1 over UTX and JMJD3. Treatment of cells with PBIT inhibits the demethylation of H3K4me3. It inhibits proliferation of breast cancer cell lines expressing high levels of JARID1B1.
1) Sayegh et al. (2013), Identification of small molecule inhibitors of Jumonji AT-rich interactive domain 1B (JARID1B) histone demethylase by a sensitive high throughput screen; J. Biol. Chem., 288 9408