GSK-J1
Based on 17 publication(s) in Google Scholar
GSK-J1, a chemical probe, is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.79%
- CAS. Nr.: 1373422-53-7
- Formel: C22H23N5O2
- Molecular Weight:389.45
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Biologische Aktivität
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Chemical Information
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Epigenetics Compound Library
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Publications Citing Use of MedChemExpress (MCE) GSK-J1
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
Biologische Aktivität
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KDM6 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
39.75 μM
Compound: GSK-J1
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Antitumor activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antitumor activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 36931124] |
| MCF7 | IC50 |
33.67 μM
Compound: GSK-J1
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Antitumor activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antitumor activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 36931124] |
| MGC-803 | IC50 |
29.31 μM
Compound: GSK-J1
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Antitumor activity against human MGC-803 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antitumor activity against human MGC-803 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 36931124] |
| PC-3 | IC50 |
20.33 μM
Compound: GSK-J1
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Antitumor activity against human PC-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antitumor activity against human PC-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 36931124] |
| Sf9 | IC50 |
16 nM
Compound: 4; GSK-J1
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Inhibition of C-terminal FLAG-tagged human KDM6B expressed in expressed in Sf9 cells pre-incubated for 4 hrs before substrate addition and measured after 1 hr by AlphaScreen assay
Inhibition of C-terminal FLAG-tagged human KDM6B expressed in expressed in Sf9 cells pre-incubated for 4 hrs before substrate addition and measured after 1 hr by AlphaScreen assay
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[PMID: 30928196] |
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. Nr. 1373422-53-7
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Appearance Solid
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Molecular Weight 389.45
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Formel C22H23N5O2
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Color White to yellow
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SMILES
OC(CCNC1=NC(C2=NC=CC=C2)=NC(N(CC3)CCC4=C3C=CC=C4)=C1)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
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 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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Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (128.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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.
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
Verweise
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5677 mL | 12.8386 mL | 25.6772 mL | 64.1931 mL |
| 5 mM | 0.5135 mL | 2.5677 mL | 5.1354 mL | 12.8386 mL | |
| 10 mM | 0.2568 mL | 1.2839 mL | 2.5677 mL | 6.4193 mL | |
| 15 mM | 0.1712 mL | 0.8559 mL | 1.7118 mL | 4.2795 mL | |
| 20 mM | 0.1284 mL | 0.6419 mL | 1.2839 mL | 3.2097 mL | |
| 25 mM | 0.1027 mL | 0.5135 mL | 1.0271 mL | 2.5677 mL | |
| 30 mM | 0.0856 mL | 0.4280 mL | 0.8559 mL | 2.1398 mL | |
| 40 mM | 0.0642 mL | 0.3210 mL | 0.6419 mL | 1.6048 mL | |
| 50 mM | 0.0514 mL | 0.2568 mL | 0.5135 mL | 1.2839 mL | |
| 60 mM | 0.0428 mL | 0.2140 mL | 0.4280 mL | 1.0699 mL | |
| 80 mM | 0.0321 mL | 0.1605 mL | 0.3210 mL | 0.8024 mL | |
| 100 mM | 0.0257 mL | 0.1284 mL | 0.2568 mL | 0.6419 mL |
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