MilliporeSigma™ Calbiochem™ Histone Lysine Demethylase Inhibitor IX, PBIT

Description

• A cell-permeable iron chelating benzisothiazolone compound with microbicide and fungicide properties that acts as a potent, selective, and reversible inhibitor of Jumonji AT-Rich Interactive Domain 1 (JARID1) histone demethylases (IC 50 = 3μM for JARID1B)
• Also blocks the activity of other related demethylases at higher concentration (IC 50 = 6, 4.9, and 28μM for JARID1A, JARID1C, and JMJD2E, respectively)
• However, it does affect the activity of unrelated UTX and JMJD3 H3K27me3 demethylases
• HeLa cells overexpressing full length JARID1B show a significant reduction in H3K4Me3 activity following PBIT treatment (∽10μM)
• Blocks the proliferation of UACC-812 tumor cells expressing higher levels of JARDID1B, but does not significantly affect MCF7 or MCF10A cells expressing lower levels of JARDID1B.