PBIT --- JARID1 Histone Demethylases Inhibitor

Bioss

PBIT --- JARID1 Histone Demethylases Inhibitor [2514-30-9]

16

Research Use Only

98.0

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 IC50 of ~3 microM in vitro. It also inhibits the activity of other related histone demethylases JARID1A, JARID1C, and JMJD2E with IC50 ~6, 4.9, and 28 microM 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 microM). 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.

-20°C

51202000