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Submit ReviewGSK J1
Description: Potent JMJD3/UTX inhibitor
Chemical Name: N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine
Purity: ≥99% (HPLC)
Biological Activity for GSK J1
GSK J1 is a potent inhibitor of the H3K27 histone demethylases JMJD3 (KDM6B) and UTX (KDM6A) (IC50 values are 28 and 53 nM respectively). Also inhibits KDM5B, KDM5C and KDM5A (IC50 values are 170, 550 and 6,800 nM respectively). Exhibits no activity against a panel of other histone demethylases (IC50 >20 μM), and displays no significant inhibitory activity against 100 protein kinases at a concentration of 30 μM.
Ethyl ester derivative and Negative Control also available.
Licensing Information
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the GSK J1 probe summary on the SGC website.
Compound Libraries for GSK J1
GSK J1 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for GSK J1
| M. Wt | 389.45 |
| Formula | C22H23N5O2 |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 1373422-53-7 |
| PubChem ID | 56963315 |
| InChI Key | AVZCPICCWKMZDT-UHFFFAOYSA-N |
| Smiles | O=C(CCNC1=NC(C2=CC=CC=N2)=NC(N3CCC(C=CC=C4)=C4CC3)=C1)O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for GSK J1
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.94 | 100 | |
| ethanol | 38.94 | 100 |
Preparing Stock Solutions for GSK J1
The following data is based on the product molecular weight 389.45. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.57 mL | 12.84 mL | 25.68 mL |
| 5 mM | 0.51 mL | 2.57 mL | 5.14 mL |
| 10 mM | 0.26 mL | 1.28 mL | 2.57 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.51 mL |
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Product Datasheets for GSK J1
References for GSK J1
References are publications that support the biological activity of the product.
Kruidenier et al (2012) A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature 488 404 PMID: 22842901
Heinemann et al (2014) Inhibition of demethylases by GSK-J1/J4. Nature 514 E1 PMID: 25279926
If you know of a relevant reference for GSK J1, please let us know.
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Keywords: GSK J1, GSK J1 supplier, GSKJ1, histone, demethylases, inhibitors, inhibits, UTX, JMJD3, H3K27, epigenetics, jumonji, demethylation, sgc, Histone, Demethylases, 4593, Tocris Bioscience
5 Citations for GSK J1
Citations are publications that use Tocris products. Selected citations for GSK J1 include:
Aspuria et al (2015) Succinate dehydrogenase inhibition leads to epithelial-mesenchymal transition and reprogrammed carbon metabolism. Nat Commun 2 21 PMID: 25671108
Lee et al (2016) Signalling couples hair follicle stem cell quiescence with reduced histone H3 K4/K9/K27me3 for proper tissue homeostasis. Cancer Metab 7 11278 PMID: 27080563
Jie et al (2021) KDM6B promotes activation of the oncogenic CDK4/6-pRB-E2F pathway by maintaining enhancer activity in MYCN-amplified neuroblastoma. Nat Commun 12 7204 PMID: 34893606
Dirk et al (2019) Targeting the H3K4 Demethylase KDM5B Reprograms the Metabolome and Phenotype of Melanoma Cells. J Invest Dermatol 139 2506-2516.e10 PMID: 31229500
Aiko et al (2020) Histone H3 K4/9/27 Trimethylation Levels Affect Wound Healing and Stem Cell Dynamics in Adult Skin. Stem Cell Reports 14 34-48 PMID: 31866458
Do you know of a great paper that uses GSK J1 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.