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PBIT is a potent, specific, reversible and cell-permeable inhibitor of Jumonji AT-Rich Interactive Domain 1 (JARID1) histone demethylases. It inhibits JARID1B (also known as KDM5B or PLU1) with an IC?? of ~3 μM in vitro. It also inhibits the activity of other related histone demethylases JARID1A, JARID1C, and JMJD2E with IC₅₀ ~6, 4.9, and 28 μM respectively. PBIT does not affect the activity of unrelated UTX and JMJD3 H3K27me3 demethylases. HeLa cells overexpressing full length JARID1B showed a significant increase in H3K4Me3 level following PBIT treatment (~10 μM). It 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.

How to Use:

• In vitro: PBIT was used at 10-30 μM in vitro.
• In vivo: n/a

Reference:

1. 1. Sayegh J, et al. Identification of small molecule inhibitors of Jumonji AT-rich interactive domain 1B (JARID1B) histone demethylase by a sensitive high throughput screen. (2013) J Biol Chem. 288(13):9408-17.