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 = 3uM for JARID1B). Also blocks the activity of other related demethylases at higher concentration (IC50 = 6, 4.9, and 28uM 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 (~10uM). 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.
Molecular Formula:C₁₄H₁₁NOS
Primary Target:JARID1 Histone Demethylases
Solubility:DMSO
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
