GSK-J4 --- H3K27 Histone Demethylases UTX and JMJD3 Inhibitor

Overview
Catalog #	bs-60063c-2mg-solid
Product Name	GSK-J4 --- H3K27 Histone Demethylases UTX and JMJD3 Inhibitor
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 417.5 Formula: C24 H27 N5 O2 CAS Number: 1373423-53-0 InChi Key: WBKCKEHGXNWYMO-UHFFFAOYSA-N InChi: InChI=1S/C24H27N5O2/c1-2-31-23(30)10-14-26-21-17-22(28-24(27-21)20-9-5-6-13-25-20)29-15-11-18-7-3-4-8-19(18)12-16-29/h3-9,13,17H,2,10-12,14-16H2,1H3,(H,26,27,28) Smiles: CCOC(=O)CCNC1C=C(N=C(N=1)C1C=CC=CN=1)N1CCC2C=CC=CC=2CC1 Purity: 98.0 Solubility: DMSO up to 100 mM Appearance: Solid Power. Shelf Life: 1.0 years
Description	GSK-J4 is an ethyl ester derivative of GSK-J1, which is the first selective and potent inhibitor of the H3K27 histone demethylases UTX and JMJD3. The highly polar carboxylate group of GSK-J1 restricts its cellular permeability, therefore GSK-J4 was developed as a pro-drug, masking the polarity of the acid group of the GSK-J1, for cellular assays. GSK-J4 could significant reduce LPS-induced pro-inflammatory cytokine production in primary human macrophages (IC50 ~9 μM for the inhibition of TNFα release). Together with GSK-J1, GSK-J4 could be a unique small molecule to allow selective pharmacological intervention across the JMJ family.