Content |
Purity≥98% |
CAS |
1797983-09-5 |
Chinese Name |
GSK-J4 盐酸盐 |
English Name |
GSK J4 Hydrochloride |
Synonym |
;GSK-J4盐酸盐;GSK-J4HCl;GSKJ4HCl;GSK-J4hydrochloride; |
Unit |
Piece |
Purity |
≥98% |
Molecular Formula |
C24H27N5O2·HCl |
Molecular Weight |
453.96 |
Appearance |
Light yellow to yellow solid |
Storage |
Powder : 2-8℃, 2 years; In solvent(mother liquid): -20℃, 1 month; -80℃, 6 months |
Solubility |
Soluble in DMSO |
MDL |
MFCD26142638 |
InChIKey |
TYXWLTBYINKVNT-UHFFFAOYSA-N |
InChI |
InChI=1S/C24H27N5O2.ClH/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);1H |
PubChem CID |
71729974 |
SMILES |
O=C(OCC)CCNC1=NC(C2=CC=CC=N2)=NC(N3CCC(C=CC=C4)=C4CC3)=C1 |
Description |
GSK J4 Hydrochloride is a potent dual inhibitor of H3K27me3/me2 demethylases JMJD3/KDM6B and UTX/KDM6A |
Target Point |
Histone Demethylase |
Passage |
Epigenetics |
IC50 |
8.6 μM (KDM6B), 6.6 μM (KDM6A)[5] |
Data Literature Source |
[1]. Kruidenier L, et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature. 2012 Aug 16;488(7411):404-8.
[2]. Donas C, et al. The histone demethylase inhibitor GSK-J4 limits inflammation through the induction of a tolerogenic phenotype on DCs. J Autoimmun. 2016 Dec;75:105-117.
[3]. Yapp C, et al. H3K27me3 demethylases regulate in vitro chondrogenesis and chondrocyte activity in osteoarthritis. Arthritis Res Ther. 2016 Jul 7;18(1):158
[4]. Kamikawa YF, et al. Histone demethylation maintains Prdm14 and Tsix expression and represses xIst in embryonic stem cells. PLoS One. 2015 May 20;10(5):e0125626
[5]. Heinemann B, et al. Inhibition of demethylases by GSK-J1/J4. Nature. 2014 Oct 2;514(7520):E1-2
[6]. Majumder S, et al. Shifts in podocyte histone H3K27me3 regulate mouse and human glomerular disease. J Clin Invest. 2018 Jan 2;128(1):483-499. |
Specification |
10mg |