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Submit ReviewGSK J4
说明： Histone KDM inhibitor; cell permeable
化学名： N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine ethyl ester
纯度： ≥99% (HPLC)
生物活性 for GSK J4
GSK J4 is a histone lysine demethylase (KDM) inhibitor; blocks demethylation of histone H3K27. Attenuates lipopolysaccharide (LPS)-induced proinflammatory cytokine production in primary human macrophages (IC50 = 9 μM for the inhibition of TNFα release). Cell permeable. Ethyl ester derivative of GSK J1.
Negative Control also available.
许可信息
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details of GSK J4, a cell permeable derivative of GSK J1, please visit the GSK J1 probe summary on the SGC website.
External Portal Information for GSK J4
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of GSK J4 is reviewed on the chemical probes website.
化合物库 for GSK J4
GSK J4 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
技术数据 for GSK J4
| 分子量 | 417.5 |
| 公式 | C24H27N5O2 |
| 储存 | Store at RT |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 1373423-53-0 |
| PubChem ID | 71729975 |
| InChI Key | WBKCKEHGXNWYMO-UHFFFAOYSA-N |
| Smiles | O=C(CCNC1=NC(C2=CC=CC=N2)=NC(N3CCC(C=CC=C4)=C4CC3)=C1)OCC |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for GSK J4
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 41.75 | 100 | |
| ethanol | 41.75 | 100 |
制备储备液 for GSK J4
以下数据基于产品分子量 417.5。 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.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.4 mL | 11.98 mL | 23.95 mL |
| 5 mM | 0.48 mL | 2.4 mL | 4.79 mL |
| 10 mM | 0.24 mL | 1.2 mL | 2.4 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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产品说明书 for GSK J4
参考文献 for GSK J4
参考文献是支持产品生物活性的出版物。
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 J4, please let us know.
按产品操作查看相关产品
关键词: GSK J4, GSK J4 supplier, GSKJ4, histone, demethylases, inhibitors, inhibits, UTX, JMJD3, KDM6, H3K27, KDMs, proinflammatory, macrophages, tnf, alpha, tnfa, anti-inflammatory, epigenetics, Histone, Demethylases, 4594, Tocris Bioscience
21 篇 GSK J4 的引用文献
引用文献是使用了 Tocris 产品的出版物。 GSK J4 的部分引用包括：
Bayo et al (2018) Jumonji Inhibitors Overcome Radioresistance in Cancer through Changes in H3K4 Methylation at Double-Strand Breaks. Cell Rep 25 1040 PMID: 30355483
Pan et al (2015) Jmjd3-Mediated H3K27me3 Dynamics Orchestrate Brown Fat Development and Regulate White Fat Plasticity. Dev Cell 35 568 PMID: 26625958
Perrigue et al (2015) The histone demethylase jumonji coordinates cellular senescence including secretion of neural stem cell-attracting cytokines. Nature 13 636 PMID: 25652587
Carey et al (2015) Intracellular α-ketoglutarate maintains the pluripotency of embryonic stem cells. Cancer Metab 518 413 PMID: 25487152
Aspuria et al (2015) Succinate dehydrogenase inhibition leads to epithelial-mesenchymal transition and reprogrammed carbon metabolism. Nat Commun 2 21 PMID: 25671108
Peter M et al (2021) Suppression of canonical TGF-β signaling enables GATA4 to interact with H3K27me3 demethylase JMJD3 to promote cardiomyogenesis. J Mol Cell Cardiol 153 44-59 PMID: 33359755
Julia et al (2021) NFAT5 Amplifies Antipathogen Responses by Enhancing Chromatin Accessibility, H3K27 Demethylation, and Transcription Factor Recruitment. J Immunol 206 2652-2667 PMID: 34031145
Alan et al (2021) Inhibition of macrophage histone demethylase JMJD3 protects against abdominal aortic aneurysms. J Exp Med 218 PMID: 33779682
Jan E et al (2021) Inhibitor of growth protein 3 epigenetically silences endogenous retroviral elements and prevents innate immune activation. Nucleic Acids Res 49 12706-12715 PMID: 34791430
Backe et al (2019) The Lysine Demethylase KDM5B Regulates Islet Function and Glucose Homeostasis. J Diabetes Res 2019 5451038 PMID: 31467927
Kang et al (2015) Transcriptomic Profiling and H3K27me3 Distribution Reveal Both Demethylase-Dependent and Independent Regulation of Developmental Gene Transcription in Cell Differentiation. PLoS One 10 e0135276 PMID: 26263556
Lin et al (2019) A KDM6A-KLF10 reinforcing feedback mechanism aggravates diabetic podocyte dysfunction. EMBO Mol Med 11 PMID: 30948420
Neal et al (2017) Structure of Nascent Chromatin Is Essential for Hematopoietic Lineage Specification. Cell Rep 19 295-306 PMID: 28402853
Kyoung Hwa et al (2017) RNA sequencing reveals resistance of TLR4 ligand-activated microglial cells to inflammation mediated by the selective jumonji H3K27 demethylase inhibitor. Sci Rep 7 6554 PMID: 28747667
Ma et al (2016) Epigenomic Regulation of Schwann Cell Reprogramming in Peripheral Nerve Injury. J Neurosci 36 9135 PMID: 27581455
Petruk et al (2013) Stepwise histone modifications are mediated by multiple enzymes that rapidly associate with nascent DNA during replication. Elife 4 2841 PMID: 24276476
Palomer et al (2016) Neuronal activity controls Bdnf expression via Polycomb de-repression and CREB/CBP/JMJD3 activation in mature neurons. Mol Cancer Res 7 11081 PMID: 27010597
Yung-Chien et al (2022) The Histone Demethylase Inhibitor GSK-J4 Is a Therapeutic Target for the Kidney Fibrosis of Diabetic Kidney Disease via DKK1 Modulation. Int J Mol Sci 23 PMID: 36012674
Steven L et al (2020) Palmitate-TLR4 signaling regulates the histone demethylase, JMJD3, in macrophages and impairs diabetic wound healing. Eur J Immunol 50 1929-1940 PMID: 32662520
Anatoly et al (2020) Combined Targeting of Mutant p53 and Jumonji Family Histone Demethylase Augments Therapeutic Efficacy of Radiation in H3K27M DIPG. Int J Mol Sci 21 PMID: 31940975
Pawel et al (2020) Bone Morphogenic Proteins Are Immunoregulatory Cytokines Controlling FOXP3+ Treg Cells. Cell Rep 33 108219 PMID: 33027660
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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.