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)
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.
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Bio/Physico-chemical Assay
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WB
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In Vivo Imaging
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IHC
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IHC
Biological Activity
Description
IC50 & Target
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KDM6 |
In Vitro
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
GSK-J1 lithium salt purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Dec 12:e13762. [Abstract]
WISH analysis of gata1a and hbbe3 expression in nap1l4a −/− and WT embryos and in embryos treated with GSK‐J1 (10 μM) at 24 hpf, and box and whisker plots show relative transcriptional levels across groups.
GSK-J1 lithium salt purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Dec 12:e13762. [Abstract]
Protein levels of H3K27me3 in nap1l4a −/− and WT embryos and in embryos treated with GSK‐J1 (10 μM) at 24 hpf, and graphs show the relative protein levels.
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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
GSK-J1 lithium salt purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Jul 26:2025.07.22.666193. [Abstract]
Morphology and number of normal eggs per well laid by virgin females treated with BATT and either GSK-J2 or GSK-J1.
GSK-J1 lithium salt purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Jul 26:2025.07.22.666193. [Abstract]
DAPI and Fast BBB staining showing the ovary (left) and vitellaria (right) of virgin females treated with BATT and either GSK-J2 or GSK-J1.
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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)