Ethyl N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alaninate hydrochloride
GSK-J4 Hydrochloride
CAS: 1797983-09-5
Molecular Formula: C24H28ClN5O2
Ethyl N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alaninate hydrochloride - Names and Identifiers
Ethyl N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alaninate hydrochloride - Physico-chemical Properties
| Molecular Formula | C24H28ClN5O2 |
| Molar Mass | 453.96442 |
| Solubility | DMSO : 62.5 mg/mL (137.68 mM; Need ultrasonic) |
| Storage Condition | under inert gas (nitrogen or Argon) at 2-8°C |
| MDL | MFCD26142638 |
| Use | GSK-J4 hydrochloride is an effective double inhibitor of H3K27me3/me2 demethylase JMJD3/KDM6B and UTX/KDM6A with IC50 of 8.6 μM and 6.6 μM respectively. GSK-J4 hydrochloride inhibited LPS-induced TNF-α production by human primary macrophages with an IC50 value of 9 μM. GSK-J4 hydrochloride are GSK-J1 cell permeability prodrugs. |
| Target | JMJD3 |
| In vitro study | GSK J4 HCl is an ethyl ester derivative of JMJD3 selective histone demethylase inhibitor GSK-J1 with an IC50 value greater than 50 μm. GSK J4 HCl was used to detect the consequences of demethylation of H3K27me3. GSK-J4 acts on human primary macrophages to inhibit the production of lipopolysaccharide-induced cytokines, including the inflammatory tumor necrosis factor (TNF). In addition, GSK-J4 inhibited lipopolysaccharide-induced loss of H3K27me3 associated with the TNF transcription start site and inhibited recruitment of RNA polymerase II. |
Ethyl N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alaninate hydrochloride - Reference
| Reference Show more | 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. |
Ethyl N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alaninate hydrochloride - Preparation solution concentration reference
| 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 |
Last Update：2024-01-02 23:10:35
Ethyl N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alaninate hydrochloride - Reference Information
| biological activity | GSK J4 HCl is a cell-permeable GSK J1 prodrug, the first selective H3K27 histone demethylase JMJD3 and UTX inhibitor, IC50 is 60 nM in cell-free test, inhibiting the demethylase activity of JMJ family. |
| Target | Value |
| JMJD3 (Cell-free assay) | 60 nM |
| Animal Model: | Eight-week-old male db/m and db/db mice on a BKS background |
| Dosage: | 10 mg/kg |
| Administration: | i.p.; thrice-weekly for 10 weeks |
| Result: | Attenuated the development of kidney disease in diabetic mice. |
Last Update：2024-04-10 22:29:15
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Product Name: GSK-J4 Hydrochloride Visit Supplier Webpage Request for quotationCAS: 1797983-09-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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Ethyl N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alaninate hydrochloride
vinylene trithiocarbonate
vinylene trithiocarbonate