GSK-J1 lithium salt
Based on 17 publication(s) in Google Scholar
GSK-J1 lithium salt is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.
For research use only. We do not sell to patients.
- Purity: 98.33%
- CAS No.: 2309668-29-7
- Formula: C22H22LiN5O2
- Molecular Weight:395.38
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GSK-J1 lithium salt
More- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- J Exp Clin Cancer Res. 2024 May 30;43(1):152. [Abstract]
- Adv Sci (Weinh). 2025 Dec 12:e13762. [Abstract]
- Acta Pharmacol Sin. 2022 Feb;43(2):457-469. [Abstract]
- Oncogene. 2021 Apr;40(15):2711-2724. [Abstract]
- Clin Exp Med. 2025 Nov 25;26(1):33. [Abstract]
- iScience. 2024 May 16;27(6):110011. [Abstract]
- Front Mol Neurosci. 2017 Mar 13;10:51. [Abstract]
- Mol Divers. 2024 Dec;28(6):4403-4424. [Abstract]
- J Chromatogr A. 2020 Feb 22;1613:460625. [Abstract]
- Mol Carcinog. 2025 Nov 18. [Abstract]
- Res Sq. 2025 Aug 12.
- bioRxiv. 2025 Jul 26:2025.07.22.666193. [Abstract]
- SSRN. 2021 Dec.
- Patent. US20200376146A1.
- Patent. US20200376102A1.
- Patent. US20180263995A1.
Customer Validation & Images
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IHC
Biological Activity
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KDM6 |
GSK-J1 is selective for H3K27 demethylases of the KDM6 subfamily and specifically binds to endogenous JMJD3. GSK-J1 inhibits TNF-α production by human primary macrophages in an H3K27-dependent manner[1]. GSK-J1 inhibits the demethylase activity of KDM5C with 8.5-fold increased potency compared with that of KDM5B at 1 mM α-ketoglutarate, with IC50 of 11 μM and 94 μM, respectively[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2309668-29-7
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Appearance Solid
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Molecular Weight 395.38
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Formula C22H22LiN5O2
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Color White to off-white
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SMILES
[Li]OC(CCNC1=NC(C2=NC=CC=C2)=NC(N(CC3)CCC4=C3C=CC=C4)=C1)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (17)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
J Exp Clin Cancer Res
Unveiling the role of HP1α-HDAC1-STAT1 axis as a therapeutic target for HP1α-positive intrahepatic cholangiocarcinoma. [Abstract]2024 May 30;43(1):152. PMID: 38812060 -
Adv Sci (Weinh)
Nap1L4a Cooperates with Scl/Klf1 to Recruit H2A.Z in Mediating Interactions Among Cis-Regulatory Elements and Transcription Required for Primitive Erythropoiesis in Zebrafish. [Abstract]2025 Dec 12:e13762. PMID: 41387107 -
Acta Pharmacol Sin
2022 Feb;43(2):457-469. PMID: 33850273 -
Oncogene
2021 Apr;40(15):2711-2724. PMID: 33712705 -
Clin Exp Med
Corin: a dual inhibitor for KDM1A/HDAC1, suppresses hepatocellular carcinoma by triggering cuproptosis. [Abstract]2025 Nov 25;26(1):33. PMID: 41286164 -
iScience
Transcriptional synergy in human aortic endothelial cells is vulnerable to combination p300/CBP and BET bromodomain inhibition. [Abstract]2024 May 16;27(6):110011. PMID: 38868181 -
Front Mol Neurosci
Inhibition of H3K27me3 Histone Demethylase Activity Prevents the Proliferative Regeneration of Zebrafish Lateral Line Neuromasts. [Abstract]2017 Mar 13;10:51. PMID: 28348517
GSK-J1 lithium salt purchased from MedChemExpress. Usage Cited in: Front Mol Neurosci. 2017 Mar 13;10:51. [Abstract]
GSK-J1 impaired zebrafish hair cell regeneration. 5 dpf larvae are treated with 400 μM Neomycin for 1 h followed by GSK-J1 exposure for 24 in the presence of BrdU. GSK-J1 significantly reduces the numbers of myosinVI-positive (green) hair cells and BrdU-positive (red) replicating cells.
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Mol Divers
Exploring host epigenetic enzymes as targeted therapies for visceral leishmaniasis: in silico design and in vitro efficacy of KDM6B and ASH1L inhibitors. [Abstract]2024 Dec;28(6):4403-4424. PMID: 38522046 -
J Chromatogr A
Screening of inhibitors against histone demethylation jumonji domain-containing protein 3 by capillary electrophoresis. [Abstract]2020 Feb 22;1613:460625. PMID: 31668999 -
Mol Carcinog
KDM6A Exhibits Antitumor Activities Toward Ovarian Cancer by Epigenetically Activating Transcription of ISG-15. [Abstract]2025 Nov 18. PMID: 41252674 -
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bioRxiv
2025 Jul 26:2025.07.22.666193. PMID: 40777373 -
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Protocol
Purified JmjD3 (1 μM) and UTX (3 μM) is incubated with 10 μM peptide [BiotinKAPRKQLATKAARK(me3 )SAPATGG] in 50 mM HEPES pH 7.5, 150 mM KCl, 50 μM (NH4)2SO4·FeSO4·H2O, 1 mM 2-oxoglutarate, and 2 mM ascorbate (JmjD3, 3 minutes at 25°C; UTX, 20 minutes at 25°C) with various concentration of the inhibitor (0, 0.005, 0.01, 0.02, 0.05, 0.1 μM). 10 mM EDTA is added to stop the reaction. The reaction is desalted by zip tip and spotted on a MALDI plate with α-cyano-4-hydroxycinnamic acid MALDI matrix. Samples are analysed on a MALDI-TOF R system.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Kruidenier L, et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature. 2012 Aug 16;488(7411):404-8. [Content Brief]
[2]. Heinemann B, et al. Inhibition of demethylases by GSK-J1/J4. Nature. 2014 Oct 2;514(7520):E1-2 [Content Brief]
[3]. Horton JR, et al. Characterization of a Linked Jumonji Domain of the KDM5/JARID1 Family of Histone H3 Lysine 4 Demethylases. J Biol Chem. 2016 Feb 5;291(6):2631-46. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GSK-J1 lithium salt Related Classifications
HY-15648D Related Classifications
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