GSK-J4 盐酸盐
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- CAS号:
- 1797983-09-5
- 英文名:
- GSK-J4 Hydrochloride
- 英文别名:
- 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;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
- 中文名:
- GSK-J4 盐酸盐
- 中文别名:
- 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
- CBNumber:
- CB12700565
- 分子式:
- C24H28ClN5O2
- 分子量:
- 453.96442
- MOL File:
- 1797983-09-5.mol
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GSK-J4 盐酸盐化学性质
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储存条件:
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under inert gas (nitrogen or Argon) at 2-8°C
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溶解度:
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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)-
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形态:
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A crystalline solid
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GSK-J4 盐酸盐性质、用途与生产工艺
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)
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60 nM
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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.
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Animal Model:
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Eight-week-old male db/m and db/db mice on a BKS background
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Dosage:
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10 mg/kg
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Administration:
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i.p.; thrice-weekly for 10 weeks
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Result:
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Attenuated the development of kidney disease in diabetic mice.
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GSK-J4 盐酸盐
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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| 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 |
1797983-09-5, GSK-J4 盐酸盐 相关搜索:
- 药靶配体
- 797983-09-5
- 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
- 化合物GSK-J4 HYDROCHLORIDE
- GSK-J4 盐酸盐
- 1797983-09-5
- 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
- Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate hydrochloride
- 1797983-09-5 (HCl)
- Ethyl N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alaninate hydrochloride
- TYXWLTBYINKVNT-UHFFFAOYSA-N
- GSK-J4 Hydrochloride