GSK-J4 盐酸盐
| 中文名称 | GSK-J4 盐酸盐 |
|---|---|
| 中文同义词 | GSK-J4 盐酸盐;化合物GSK-J4 HYDROCHLORIDE;3-((6-(4,5-二氢-1H-苯并[D]氮杂庚烷-3(2H)-基)-2-(吡啶-2-基)嘧啶-4-基)氨基)丙酸乙酯盐酸盐 |
| 英文名称 | GSK-J4 Hydrochloride |
| 英文同义词 | 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;1797983-09-5 (HCl);Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate hydrochloride;Histone Demethylase,diabetic,Th17,mice,cells,inflammation,Th1,H3K27me3/me2,dendritic,GSKJ4 Hydrochloride,TGF-β,inhibit,Inhibitor,GSK J4 Hydrochloride,demethylase,GSK-J4,GSK-J-4 Hydrochloride |
| CAS号 | 1797983-09-5 |
| 分子式 | C24H28ClN5O2 |
| 分子量 | 453.96442 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1797983-09-5.mol |
| 结构式 |  |
GSK-J4 盐酸盐 性质
| 储存条件 | under inert gas (nitrogen or Argon) at 2-8°C |
|---|---|
| 溶解度 | DMSO:60.83(Max Conc. mg/mL);134.0(Max Conc. mM) DMSO:PBS (pH 7.2) (1:7):0.1(Max Conc. mg/mL);0.22(Max Conc. mM) DMF:30.0(Max Conc. mg/mL);66.08(Max Conc. mM) Ethanol:55.0(Max Conc. mg/mL);121.15(Max Conc. mM) Water:10.0(Max Conc. mg/mL);22.03(Max Conc. mM) |
| 形态 | 结晶固体 |
| 颜色 | 浅黄至黄色 |
GSK J4 HCl是一种细胞渗透性的GSK J1前体药物，是第一个选择性H3K27组蛋白去甲基化酶JMJD3和UTX抑制剂，无细胞试验中IC50为60 nM，抑制JMJ家族的去甲基化酶活性。
| Target | Value |
|
JMJD3
(Cell-free assay) | 60 nM |
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。
GSK-J4 Hydrochloride (10 mg/kg; i.p.; thrice-weekly for 10 weeks) attenuates the development of kidney disease in diabetic mice.
GSK-J4 Hydrochloride (0.5 mg/kg, i.p.) significantly reduces the severity and delays the onset of the disease of the mouse model of experimental autoimmune encephalomyelitis.
| 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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-15648F | GSK-J4 hydrochloride | 5 mg | 750元 | |
| 2024/04/30 | HY-15648F | GSK-J4 盐酸盐 GSK-J4 hydrochloride | 1797983-09-5 | 10mg | 1200元 |