GSK-J4
GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable proagent of GSK-J1[1][2][3]. GSK-J4 induces endoplasmic reticulum stress-related apoptosis[4].
Product Specifications
CAS Number
[1373423-53-0]
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Apoptosis; Histone Demethylase
Type
Reference compound
Related Pathways
Apoptosis; Epigenetics
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/GSK-J4.html
Purity
99.45
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
O=C(OCC)CCNC1=NC(C2=CC=CC=N2)=NC(N3CCC(C=CC=C4)=C4CC3)=C1
Molecular Formula
C24H27N5O2
Molecular Weight
417.50
Precautions
H302, H315, H319, H335
References & Citations
[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.|[7]Xuan Chu, et al. GSK-J4 induces cell cycle arrest and apoptosis via ER stress and the synergism between GSK-J4 and decitabine in acute myeloid leukemia KG-1a cells. Cancer Cell International volume 20, Article number: 209 (2020) .
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
KDM6
Citation 01
Adv Sci (Weinh) . 2023 Aug;10 (22) :e2206798.|Biochem J. 2019 Jun 26;476 (12) :1741-1751.|Biochim Biophys Acta Mol Cell Biol Lipids. 2021 Jun;1866 (6) :158901.|Biomed Res Int. 2020 Mar 18;2020:2953068.|bioRxiv. 2023 Apr 3.|bioRxiv. 2024 August 09.|bioRxiv. 2024 July 27.|biorxiv. 2024 Jun 03.|bioRxiv. 2025 Jul 12:2025.07.08.663754.|bioRxiv. 2025 Jul 21.|bioRxiv. 2025 Oct 14.|Br J Pharmacol. 2023 Sep;180 (17) :2250-2265.|Cancer Cell Int. 2020 Jun 3;20:209.|Cell Commun Signal. 2022 Oct 27;20 (1) :168.|Cell Death Dis. 2023 Aug 15;14 (8) :520.|Cell Death Dis. 2025 Nov 3;16 (1) :782.|Cell Death Discov. 2023 Nov 14;9 (1) :413.|Cell Signal. 2023 May:105:110626.|Clin Epigenetics. 2024 Jan 20;16 (1) :14.|Clin Exp Med. 2025 Nov 25;26 (1) :33.|Commun Biol. 2022 Sep 2;5 (1) :904.|Ecotoxicol Environ Saf. 2025 Feb 6:291:117847.|EMBO Rep. 2024 Dec;25 (12) :5429-5455.|Exp Cell Res. 2020 Oct 15;395 (2) :112173.|Free Radic Biol Med. 2024 Jan:210:462-477.|Front Cardiovasc Med. 2022 Jun 2;9:907747.|Gene. 2022 May 15:822:146317.|Genes (Basel) . 2020 Apr 30;11 (5) :495.|Immunity. 2024 May 14;57 (5) :1087-1104.e7.|Invest Ophthalmol Vis Sci. 2024 Feb 1;65 (2) :34.|iScience. 2024 May 16.|IUBMB Life. 2019 Nov;71 (11) :1711-1719.|J Biomed Mater Res A. 2025 Jan;113 (1) :e37861.|J Biomed Sci. 2025 Jan 13;32 (1) :8.|J Clin Invest. 2018 Jan 2;128 (1) :483-499. |J Proteome Res. 2024 Apr 5;23 (4) :1495-1505.|Mol Divers. 2024 Dec;28 (6) :4403-4424.|Mol Metab. 2025 Apr:94:102113.|Nat Commun. 2023 Jan 20;14 (1) :336.|Neoplasia. 2025 Oct:68:101223.|Oncol Rep. 2019 May;41 (5) :2667-2678.|Patent. US20180263995A1.|Patent. US20200376102A1.|Patent. US20200376146A1.|Research Square Preprint. 2020 Jul.|Research Square Preprint. 2020 Nov.|Research Square Preprint. 2022 Feb.|Research Square Preprint. 2022 Jul.|Sci Adv. 2021 Mar 5;7 (10) :eabe7853.|Stem Cell Res Ther. 2024 Nov 15;15 (1) :431.|Transl Oncol. 2025 Jan 14:52:102271.|University of Kentucky. Toxicology and Cancer Biology. 2021 May.|University of New York|Clin Exp Med. 2025 Nov 25;26 (1) :33.
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