Histone Lysine Demethylase Inhibitor IX, PBIT

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 (IC₅₀ = 3 µM for JARID1B). Also blocks the activity of other related demethylases at higher concentration (IC₅₀ = 6, 4.9, and 28 µM 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 (~10 µM). 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.

Cell permeable: yes

Primary Target
JARID1 Histone Demethylases

Reversible: yes

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Use only fresh DMSO for reconstitution.

Sayegh, J., et al. 2013. J. Biol. Chem.288, 9408.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany