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Submit ReviewGSK J1
说明： Potent JMJD3/UTX inhibitor
化学名： N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine
纯度： ≥99% (HPLC)
生物活性 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.
许可信息
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.
化合物库 for GSK J1
GSK J1 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for GSK J1
| 分子量 | 389.45 |
| 公式 | C22H23N5O2 |
| 储存 | Desiccate at RT |
| 纯度 | ≥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 |
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 J1
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 38.94 | 100 | |
| ethanol | 38.94 | 100 |
制备储备液 for GSK J1
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for GSK J1
参考文献 for GSK J1
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 J1, please let us know.
按产品操作查看相关产品
关键词: GSK J1, GSK J1 supplier, GSKJ1, histone, demethylases, inhibitors, inhibits, UTX, JMJD3, H3K27, epigenetics, jumonji, demethylation, sgc, Histone, Demethylases, 4593, Tocris Bioscience
5 篇 GSK J1 的引用文献
引用文献是使用了 Tocris 产品的出版物。 GSK J1 的部分引用包括：
Aspuria et al (2015) Succinate dehydrogenase inhibition leads to epithelial-mesenchymal transition and reprogrammed carbon metabolism. Nat Commun 2 21 PMID: 25671108
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
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
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
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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.