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81379
PBIT
Activators & Inhibitors
Chemical Modulators

PBIT #81379

Citations (0)
Chemical structure of PBIT.

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.

Product Description

Molecular Weight 241.3 g/mol
Purity >98%
Molecular Formula C14H11NOS
CAS 2514-30-9
Solubility Soluble in DMSO at 24 mg/mL or ethanol at 5 mg/mL.

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).

Limited Uses

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Products are labeled with For Research Use Only or a similar labeling statement and have not been approved, cleared, or licensed by the FDA or other regulatory foreign or domestic entity, for any purpose. Customer shall not use any Product for any diagnostic or therapeutic purpose, or otherwise in any manner that conflicts with its labeling statement. Products sold or licensed by CST are provided for Customer as the end-user and solely for research and development uses. Any use of Product for diagnostic, prophylactic or therapeutic purposes, or any purchase of Product for resale (alone or as a component) or other commercial purpose, requires a separate license from CST. Customer shall (a) not sell, license, loan, donate or otherwise transfer or make available any Product to any third party, whether alone or in combination with other materials, or use the Products to manufacture any commercial products, (b) not copy, modify, reverse engineer, decompile, disassemble or otherwise attempt to discover the underlying structure or technology of the Products, or use the Products for the purpose of developing any products or services that would compete with CST products or services, (c) not alter or remove from the Products any trademarks, trade names, logos, patent or copyright notices or markings, (d) use the Products solely in accordance with CST Product Terms of Sale and any applicable documentation, and (e) comply with any license, terms of service or similar agreement with respect to any third party products or services used by Customer in connection with the Products.

For Research Use Only. Not for Use in Diagnostic Procedures.
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To Purchase # 81379
Cat. # Size Qty. Price
81379S
5 mg