1797983-09-5
中文名稱
GSK-J4 鹽酸鹽
英文名稱
GSK-J4 Hydrochloride
CAS
1797983-09-5
分子式
C24H28ClN5O2
分子量
453.964
MOL 文件
1797983-09-5.mol
更新日期
2024/06/25 17:16:03
1797983-09-5 結(jié)構(gòu)式
基本信息
中文別名
GSK-J4 鹽酸鹽化合物GSK-J4 HYDROCHLORIDE
英文別名
GSK-J4 HydrochlorideTYXWLTBYINKVNT-UHFFFAOYSA-N
Ethyl N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alaninate hydrochloride
物理化學(xué)性質(zhì)
儲(chǔ)存條件Inert atmosphere,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)
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)
形態(tài)結(jié)晶固體
顏色Light yellow to yellow
GSK-J4 鹽酸鹽價(jià)格(試劑級(jí))
| 報(bào)價(jià)日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
| 2024/11/08 | 46800 | GSK-J4 hydrochloride, 95% GSK-J4 hydrochloride, 95% | 1797983-09-5 | 100mg | 12292元 |
| 2024/11/08 | S7070 | GSK-J4 鹽酸鹽 GSK J4 HCl (GSKJ4 HCl) | 1797983-09-5 | 10mg | 1389.07元 |
| 2024/11/08 | S7070 | GSK-J4 鹽酸鹽 GSK J4 HCl (GSKJ4 HCl) | 1797983-09-5 | 10mM(1mL in DMSO) | 1799.49元 |
常見問題列表
生物活性
GSK J4 HCl是一種細(xì)胞滲透性的GSK J1前體藥物，是第一個(gè)選擇性H3K27組蛋白去甲基化酶JMJD3和UTX抑制劑，無細(xì)胞試驗(yàn)中IC50為60 nM，抑制JMJ家族的去甲基化酶活性。靶點(diǎn)
| Target | Value |
|
JMJD3
(Cell-free assay) | 60 nM |
體外研究
GSK J4 HCl是JMJD3選擇性組蛋白去甲基化酶抑制劑GSK-J1的乙酯類衍生物，IC50值大于50 μM。GSK J4 HCl用于探測H3K27me3去甲基化造成的后果。GSK-J4作用于人類原代巨噬細(xì)胞，抑制脂多糖誘導(dǎo)的細(xì)胞因子的產(chǎn)生，包括致炎的腫瘤壞死因子（TNF）。此外，GSK-J4抑制脂多糖誘導(dǎo)的與TNF轉(zhuǎn)錄起始位點(diǎn)相關(guān)的H3K27me3損失，并抑制RNA聚合酶II的招募。
體內(nèi)研究
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. |