Description
Product Usage Information
PBIT is supplied as a lyophilized powder. For a 10 mM stock, reconstitute 1 mg of powder in 0.41 mL of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.
Storage
Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles .
Background
PBIT is a small-molecule inhibitor of lysine demethylase 5B (JARID1B or KDM5B), which demethylates Lys4 of histone H3. PBIT is also involved in cell fate decisions and is overexpressed in a variety of human cancers (1). PBIT inhibits JARID1B (IC of approximately 3 μM) and the related JARID1A and JARID1C demethylases less potently (IC of 6 and 4.9 μM, respectively). PBIT treatment of breast cancer cells increased lysine methylated histone H3 protein levels, suggesting that PBIT inhibits JARID1B demethylase (2). In a study of angiotensin II-induced endothelial dysfunction in mice, inhibition of JARID1B by PBIT reduced the inflammatory response and prevented the development of endothelial dysfunction (3). Overexpression of JARID1B in non-small cell lung cancer correlated with tumor size, lymph node metastasis, advanced stages, and poor overall survival; inhibition of JARID1B by PBIT enhanced cancer cell death and increased treatment effectiveness (4).
Alternate Names
2-(4-Methylphenyl)-1,2-benzisothiazol-3(2H)-one
