中文名 | GSK-J4 HCl |
英文名 | GSK-J4 Hydrochloride |
别名 | GSK-J4 盐酸盐 化合物GSK-J4 HYDROCHLORIDE |
英文别名 | GSK-J4 HCl 1797983-09-5 (HCl) GSK-J4 Hydrochloride TYXWLTBYINKVNT-UHFFFAOYSA-N Ethyl N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alaninate hydrochloride |
CAS | 1797983-09-5 |
化学式 | C24H28ClN5O2 |
分子量 | 453.96442 |
溶解度 | DMSO: 62.5毫克/毫升 (137.68毫米; 需要超声波) |
存储条件 | under inert gas (nitrogen or Argon) at 2-8°C |
MDL号 | MFCD26142638 |
靶点 | JMJD3 |
体外研究 | GSK J4 HCl是JMJD3选择性组蛋白去甲基化酶抑制剂GSK-J1的乙酯类衍生物,IC50值大于50 μM。GSK J4 HCl用于探测H3K27me3去甲基化造成的后果。GSK-J4作用于人类原代巨噬细胞,抑制脂多糖诱导的细胞因子的产生,包括致炎的肿瘤坏死因子(TNF)。此外,GSK-J4抑制脂多糖诱导的与TNF转录起始位点相关的H3K27me3损失,并抑制RNA聚合酶II的招募。 |
参考资料 展开查看 | 1: Wu W, Qin M, Jia W, Huang Z, Li Z, Yang D, Huang M, Xiao C, Long F, Mao J, Moore PK, Liu X, Zhu YZ. Cystathionine-γ-lyase ameliorates the histone demethylase JMJD3-mediated autoimmune response in rheumatoid arthritis. Cell Mol Immunol. 2018 May 29. doi: 10.1038/s41423-018-0037-8. [Epub ahead of print] PubMed PMID: 29844591. 2: Daures M, Idrissou M, Judes G, Rifaï K, Penault-Llorca F, Bignon YJ, Guy L, Bernard-Gallon D. A new metabolic gene signature in prostate cancer regulated by JMJD3 and EZH2. Oncotarget. 2018 May 4;9(34):23413-23425. doi: 10.18632/oncotarget.25182. eCollection 2018 May 4. PubMed PMID: 29805743; PubMed Central PMCID: PMC5955128. 3: Lochmann TL, Powell KM, Ham J, Floros KV, Heisey DAR, Kurupi RIJ, Calbert ML, Ghotra MS, Greninger P, Dozmorov M, Gowda M, Souers AJ, Reynolds CP, Benes CH, Faber AC. Targeted inhibition of histone H3K27 demethylation is effective in high-risk neuroblastoma. Sci Transl Med. 2018 May 16;10(441). pii: eaao4680. doi: 10.1126/scitranslmed.aao4680. PubMed PMID: 29769286. 4: Guo Z, Lu J, Li J, Wang P, Li Z, Zhong Y, Guo K, Wang J, Ye J, Liu P. JMJD3 inhibition protects against isoproterenol-induced cardiac hypertrophy by suppressing β-MHC expression. Mol Cell Endocrinol. 2018 May 10. pii: S0303-7207(18)30157-6. doi: 10.1016/j.mce.2018.05.009. [Epub ahead of print] PubMed PMID: 29753027. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.203 ml | 11.014 ml | 22.028 ml |
5 mM | 0.441 ml | 2.203 ml | 4.406 ml |
10 mM | 0.22 ml | 1.101 ml | 2.203 ml |
5 mM | 0.044 ml | 0.22 ml | 0.441 ml |
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