PBIT

Aliases: PBIT, 2-(4-Methylphenyl)-1,2-benzisothiazol-3(2H)-one
Catalog No: 14110 Format: 25 mg $235 Buy
Catalog No: 14111 Format: 5 mg $65 Buy
Application: Histone Methylation (HMT & HDM)

Chemical Properties

MW = 241.3
C14H11NOS
CAS 2514-30-9
>98% (TLC); NMR (Conforms)

Description

The JARID1 (Jumonji AT-Rich Interactive Domain 1) family of lysine demethylases is responsible for demethylation of trimethylated lysine 4 in histone H3 (H3K4me3). PBIT is a potent and selective inhibitor of JARID1 (IC50 = 3, 4.9 and 6 µM for JARID1B, 1A and 1C, respectively). Selective for JARID1 over UTX and JMJD3. Treatment of cells with PBIT inhibits the demethylation of H3K4me3. It inhibits proliferation of breast cancer cell lines expressing high levels of JARID1B (ref 1).

Contents

Off-white powder. May be dissolved in DMSO (24 mg/ml); or ethanol (5 mg/ml).

Storage Conditions

Store desiccated as supplied at -20°C for up to 2 years. Store solutions at -20°C for up to 1 month.

References

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

 
Chemical structure of PBIT.

Chemical structure of PBIT.