| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C22H22LiN5O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
GSK-J1 lithium salt is a potent inhibitor of the H3K27me3/me2 demethylases JMJD3/KDM6B and UTX/KDM6A, with an IC50 of 60 nM toward KDM6B. It is supplied as a white to off-white solid (C22H22LiN5O2, MW 395.38) at 98.33% purity.
Physical & Chemical Properties
| CAS Number | 2309668-29-7 |
|---|---|
| Molecular Formula | C22H22LiN5O2 |
| Molecular Weight | 395.38 g/mol |
| Purity | 98.33% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | [Li]OC(CCNC1=NC(C2=NC=CC=C2)=NC(N(CC3)CCC4=C3C=CC=C4)=C1)=O |
| Target | KDM6 |
| Signaling Pathway | Epigenetics |
| Storage | 4°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[2]. Heinemann B, et al. Inhibition of demethylases by GSK-J1/J4. Nature. 2014 Oct 2;514(7520):E1-2
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
GSK-J1 selectively targets the KDM6 subfamily of H3K27 demethylases and binds specifically to endogenous JMJD3. In human primary macrophages, GSK-J1 suppresses TNF-α production in an H3K27-dependent manner[1]. At 1 mM α-ketoglutarate, GSK-J1 inhibits KDM5C demethylase activity with 8.5-fold greater potency than KDM5B, with IC50 values of 11 μM and 94 μM, respectively[3].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. Nat Commun 2026 Feb 12;17(1):1214. PMID: 41680175
Unveiling the role of HP1α-HDAC1-STAT1 axis as a therapeutic target for HP1α-positive intrahepatic cholangiocarcinoma. J Exp Clin Cancer Res 2024 May 30;43(1):152. PMID: 38812060
Nap1L4a Cooperates with Scl/Klf1 to Recruit H2A.Z in Mediating Interactions Among Cis-Regulatory Elements and Transcription Required for Primitive Erythropoiesis in Zebrafish. Adv Sci (Weinh) 2025 Dec 12:e13762. PMID: 41387107
P300/CBP inhibition sensitizes mantle cell lymphoma to PI3Kδ inhibitor idelalisib. Acta Pharmacol Sin 2022 Feb;43(2):457-469. PMID: 33850273
BRD4 inhibition sensitizes cervical cancer to radiotherapy by attenuating DNA repair. Oncogene 2021 Apr;40(15):2711-2724. PMID: 33712705
Corin: a dual inhibitor for KDM1A/HDAC1, suppresses hepatocellular carcinoma by triggering cuproptosis. Clin Exp Med 2025 Nov 25;26(1):33. PMID: 41286164
Transcriptional synergy in human aortic endothelial cells is vulnerable to combination p300/CBP and BET bromodomain inhibition. iScience 2024 May 16;27(6):110011. PMID: 38868181
Inhibition of H3K27me3 Histone Demethylase Activity Prevents the Proliferative Regeneration of Zebrafish Lateral Line Neuromasts. Front Mol Neurosci 2017 Mar 13:10:51.
Exploring host epigenetic enzymes as targeted therapies for visceral leishmaniasis: in silico design and in vitro efficacy of KDM6B and ASH1L inhibitors. Mol Divers 2024 Dec;28(6):4403-4424. PMID: 38522046
Screening of inhibitors against histone demethylation jumonji domain-containing protein 3 by capillary electrophoresis. J Chromatogr A 2020 Feb 22:1613:460625. PMID: 31668999
