GSK-J4 free base

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 555282

CAS#: 1373423-53-0 (free base)

Description: GSK-J4 is a cell permeable, potent and selective histone demethylase. GSK-J4 is a prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family. GSK-J4 is used to probe the consequences of demethylation of H3K27me3. GSK-J4 inhibits the lipopolysaccharide-induced production of cytokines, including pro-inflammatory tumour necrosis factor (TNF).

Price and Availability

Size Price Shipping out time Quantity
100mg USD 950 2 Weeks
200mg USD 1450 2 Weeks
500mg USD 2450 2 Weeks
1g USD 3450 2 Weeks
2g USD 5450 2 Weeks
5g USD 8450 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-01-24. Prices are subject to change without notice.

GSK-J4 free base, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Chemical Structure


Theoretical Analysis

MedKoo Cat#: 555282
Name: GSK-J4 free base
CAS#: 1373423-53-0 (free base)
Chemical Formula: C24H27N5O2
Exact Mass: 417.2165
Molecular Weight: 417.513
Elemental Analysis: C, 69.04; H, 6.52; N, 16.77; O, 7.66

Related CAS #: 1797983-09-5 (HCl)   1373423-53-0 (free base)    

Synonym: GSK-J4 free base; GSK-J-4; GSK-J 4; GSK-J4;

IUPAC/Chemical Name: ethyl 3-((2-(pyridin-2-yl)-6-(1,2,4,5-tetrahydro-3H-benzo[d]azepin-3-yl)pyrimidin-4-yl)amino)propanoate


InChi Code: 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)


Technical Data

Solid powder

>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Soluble in DMSO

Shelf Life:
>3 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:


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4: Guo Z, Lu J, Li J, Wang P, Li Z, Zhong Y, Guo K, Wang J, Ye J, Liu P. JMJD3 inhibition protects against isoproterenol-induced cardiac hypertrophy by suppressing β-MHC expression. Mol Cell Endocrinol. 2018 May 10. pii: S0303-7207(18)30157-6. doi: 10.1016/j.mce.2018.05.009. [Epub ahead of print] PubMed PMID: 29753027.

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7: Jia W, Wu W, Yang D, Xiao C, Su Z, Huang Z, Li Z, Qin M, Huang M, Liu S, Long F, Mao J, Liu X, Zhu YZ. Histone demethylase JMJD3 regulates fibroblast-like synoviocyte-mediated proliferation and joint destruction in rheumatoid arthritis. FASEB J. 2018 Jul;32(7):4031-4042. doi: 10.1096/fj.201701483R. Epub 2018 Feb 26. PubMed PMID: 29481307.

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10: Rejlova K, Musilova A, Kramarzova KS, Zaliova M, Fiser K, Alberich-Jorda M, Trka J, Starkova J. Low HOX gene expression in PML-RARα-positive leukemia results from suppressed histone demethylation. Epigenetics. 2018;13(1):73-84. doi: 10.1080/15592294.2017.1413517. Epub 2018 Feb 7. PubMed PMID: 29224413; PubMed Central PMCID: PMC5836981.

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13: Sui A, Xu Y, Li Y, Hu Q, Wang Z, Zhang H, Yang J, Guo X, Zhao W. The pharmacological role of histone demethylase JMJD3 inhibitor GSK-J4 on glioma cells. Oncotarget. 2017 Aug 2;8(40):68591-68598. doi: 10.18632/oncotarget.19793. eCollection 2017 Sep 15. PubMed PMID: 28978140; PubMed Central PMCID: PMC5620280.

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16: Yan N, Xu L, Wu X, Zhang L, Fei X, Cao Y, Zhang F. GSKJ4, an H3K27me3 demethylase inhibitor, effectively suppresses the breast cancer stem cells. Exp Cell Res. 2017 Oct 15;359(2):405-414. doi: 10.1016/j.yexcr.2017.08.024. Epub 2017 Aug 18. PubMed PMID: 28823831.

17: Das A, Arifuzzaman S, Yoon T, Kim SH, Chai JC, Lee YS, Jung KH, Chai YG. RNA sequencing reveals resistance of TLR4 ligand-activated microglial cells to inflammation mediated by the selective jumonji H3K27 demethylase inhibitor. Sci Rep. 2017 Jul 26;7(1):6554. doi: 10.1038/s41598-017-06914-5. PubMed PMID: 28747667; PubMed Central PMCID: PMC5529413.

18: Backe MB, Andersson JL, Bacos K, Christensen DP, Hansen JB, Dorosz JJ, Gajhede M, Dahlby T, Bysani M, Kristensen LH, Ling C, Olsen L, Mandrup-Poulsen T. Lysine demethylase inhibition protects pancreatic β cells from apoptosis and improves β-cell function. Mol Cell Endocrinol. 2018 Jan 15;460:47-56. doi: 10.1016/j.mce.2017.07.001. Epub 2017 Jul 4. PubMed PMID: 28684291.

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20: Ha SD, Cho W, Kim SO. HDAC8 Prevents Anthrax Lethal Toxin-induced Cell Cycle Arrest through Silencing PTEN in Human Monocytic THP-1 Cells. Toxins (Basel). 2017 May 16;9(5). pii: E162. doi: 10.3390/toxins9050162. PubMed PMID: 28509866; PubMed Central PMCID: PMC5450710.