GSK J1

Catalog No.S7581 Batch:S758102

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Technical Data

Formula

C22H23N5O2
Molecular Weight 389.45 CAS No. 1373422-53-7
Solubility (25°C)* In vitro DMSO 77 mg/mL (197.71 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description GSK-J1 is a highly potent inhibitor of H3K27 histone demethylase JMJD3 (KDM6B) and UTX (KDM6A) with IC50 of 60 nM in cell-free assays for JMJD3 (KDM6B) , respectively, >10-fold selectivity over other tested demethylases, with IC50 of 0.95μM and 1.76μM towards JARID1B/C.
Targets
JMJD3 [1]
60 nM
In vitro

In HEK-293 cells, GSK-J1 inhibits the activities of transiently transfected JMJD3 and UTX. GSK-J1 also inhibits TNF-α production by human primary macrophages by increasing total nuclear H3K27me3 levels. [1]

In MC3T3-E1 cells, GSK-J1 suppresses Runx2 and Osterix expressions and ALP activity, and increases the global levels of H3K27me3. [2]
In vivo

GSK-J1, a small molecule inhibitor of JMJD3, directly interfered with the transcription of inflammatory-related genes by H3K27me3 modification of their promoters.

Protocol (from reference)

Kinase Assay:

[1]
  • MALDI-TOF Analysis of JmjD3 and UTX Activity

    Purified JmjD3 (1 μM) and UTX (3 μM) is incubated with 10 μM peptide [Biotin-KAPRKQLATKAARK(me3)SAPATGG] in 50 mM HEPES pH 7.5, 150 mM KCl, 50μM (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). 10mM 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.

Selleck's GSK J1 has been cited by 11 publications

Dysregulated Gln-Glu-α-ketoglutarate axis impairs maternal decidualization and increases the risk of recurrent spontaneous miscarriage [ Cell Rep Med, 2023, 4(5):101026] PubMed: 37137303
Systematic identification of biomarker-driven drug combinations to overcome resistance [ Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7] PubMed: 35332332
The JMJD3 histone demethylase inhibitor GSK-J1 ameliorates lipopolysaccharide-induced inflammation in a mastitis model [ J Biol Chem, 2022, S0021-9258(22)00457-4] PubMed: 35526564
Asxl1 C-terminal mutation perturbs neutrophil differentiation in zebrafish [ Leukemia, 2021, 10.1038/s41375-021-01121-8] PubMed: 33483612
Depletion of Demethylase KDM6 Enhances Early Neuroectoderm Commitment of Human PSCs [ Front Cell Dev Biol, 2021, 9:702462] PubMed: 34568320
Therapeutic effect of a histone demethylase inhibitor in Parkinson's disease [ Cell Death Dis, 2020, 11(10):927] PubMed: 33116116
Early secreted antigenic target of 6-kDa of Mycobacterium tuberculosis induces transition of macrophages into epithelioid macrophages by downregulating iNOS / NO-mediated H3K27 trimethylation in macrophages. [ Mol Immunol, 2020, 117:189-200] PubMed: 31816492
An epitranscriptomic mechanism underlies selective mRNA translation remodelling in melanoma persister cells. [ Nat Commun, 2019, 10(1):5713] PubMed: 31844050
Negative regulation of miR-1275 by H3K27me3 is critical for glial induction of glioblastoma cells. [ Mol Oncol, 2019, 13(7):1589-1604] PubMed: 31162799
Epigenetic Reprogramming with Antisense Oligonucleotides Enhances the Effectiveness of Androgen Receptor Inhibition in Castration-Resistant Prostate Cancer [ Cancer Res, 2018, 78(20):5731-5740] PubMed: 30135193

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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