PBIT (#81379) Datasheet Without Images Cell Signaling Technology

For Research Use Only. Not for Use in Diagnostic Procedures.

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 (IC₅₀ of approximately 3 μM) and the related JARID1A and JARID1C demethylases less potently (IC₅₀ 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 in vivo (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).

Molecular Formula

C₁₄H₁₁NOS

Molecular Weight

241.3 g/mol

Purity

>98%

CAS

2514-30-9

Solubility

Soluble in DMSO at 24 mg/mL or ethanol at 5 mg/mL.

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.

Directions for Use

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.

Background References

Cross-Reactivity Key

H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected

Trademarks and Patents

Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.

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