GSK J1

製品コードS7581 バッチS758104

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C22H23N5O2
分子量 389.45 CAS No. 1373422-53-7
Solubility (25°C)* 体外 DMSO 78 mg/mL (200.28 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 GSK-J1 is a highly potent H3K27 histone demethylase inhibitor with IC50 of 28 nM and 53 nM in cell-free assays for JMJD3 (KDM6B) and UTX (KDM6A), respectively, >10-fold selectivity over other tested demethylases.
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.

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 細胞株 Cell-free assays
濃度 60 nM
反応時間
実験の流れ
動物実験 動物モデル Pregnant BALB/c mice
投薬量 1 mg/kg
投与方法 i.p.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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