PBIT --- JARID1 Histone Demethylases Inhibitor

Overview
Catalog #	bs-60170c-2-mg-solid
Product Name	PBIT --- JARID1 Histone Demethylases Inhibitor
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 241.31 Formula: C14 H11 N O S CAS Number: 2514-30-9 InChi Key: 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) Smiles: CC1C=CC(=CC=1)C1=CC=CC2SNC(=O)C=21 Purity: 98.0 Solubility: DMSO up to 50 mM Appearance: Solid Power. Shelf Life: 1.0 years
Description	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.