PBIT, JARID1 Histone Demethylases Inhibitor

PBIT is a potent, specific, reversible and cell-permeable inhibitor of Jumonji AT-Rich Interactive Domain 1 (JARID1) histone demethylases. It inhibits JARID1B (also known as KDM5B or PLU1) with an IC₅₀ of ~3 μM in vitro. It also inhibits the activity of other related histone demethylases JARID1A, JARID1C, and JMJD2E with IC50 ~6, 4.9, and 28 µM respectively. PBIT does not affect the activity of unrelated UTX and JMJD3 H3K27me3 demethylases. HeLa cells overexpressing full length JARID1B showed a significant increase in H3K4Me3 level following PBIT treatment (~10 µM). It blocks the proliferation of UACC-812 tumor cells expressing higher levels of JARDID1B, but does not significantly affect MCF7 or MCF10A cells expressing lower levels of JARDID1B.

Product information

CAS Number: 2514-30-9

Molecular Weight: 241.31

Formula: C14H11NOS

Chemical Name: 2-4(4-methylphenyl)-1,2-benzisothiazol-3(2H)-one

Smiles: CC1C=CC(=CC=1)C1=CC=CC2SNC(=O)C=21

InChiKey: INRCAEDSTPYYET-UHFFFAOYSA-N

InChi: InChI=1S/C14H11NOS/c1-9-5-7-10(8-6-9)11-3-2-4-12-13(11)14(16)15-17-12/h2-8H,1H3,(H,15,16)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 50 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

PBIT was used at 10-30 µM in vitro.

References:

1. Sayegh J, et al. Identification of small molecule inhibitors of Jumonji AT-rich interactive domain 1B (JARID1B) histone demethylase by a sensitive high throughput screen. (2013) J Biol Chem. 288(13):9408-17.

Products are for research use only. Not for human use.