PBIT, JARID1 inhibitor (TBI1595)

Description

Product Details

Formal Name: 2-(4-Methylphenyl)-1,2-benzisothiazol-3(2H)-one

Molecular Formula: C₁₄H₁₁NOS

Formula Weight: 241.31

CAS Number: 2514-30-9

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 24 mg/ml) or in Ethanol (up to 5 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

JARID1 inhibitor

Functions

The JARID1 (Jumonji AT-Rich Interactive Domain 1) family of lysine demethylases demethylates the trimethylated lysine 27 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 JARID1B1.

Application Procedures

First dissolved in DMSO (up to 24 mg/ml) or in Ethanol (up to 5 mg/ml), then diluted to aqueous buffer. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.