GSK-J4 鹽酸鹽
| 中文名稱 | GSK-J4 鹽酸鹽 |
|---|---|
| 中文同義詞 | GSK-J4 鹽酸鹽;化合物GSK-J4 HYDROCHLORIDE;3-((6-(4,5-二氫-1H-苯并[D]氮雜庚烷-3(2H)-基)-2-(吡啶-2-基)嘧啶-4-基)氨基)丙酸乙酯鹽酸鹽;N-[2-(2-吡啶基)-6-(1,2,4,5-四氫-3H-3-苯并氮雜-3-基)-4-嘧啶基]-BETA-丙氨酸乙酯鹽酸鹽;化合物GSK-J4 HYDROCHLORIDE,10 MM DMSO 溶液 |
| 英文名稱 | GSK-J4 Hydrochloride |
| 英文同義詞 | 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;GSK-J4 Hydrochloride, 10 mM in DMSO |
| CAS號 | 1797983-09-5 |
| 分子式 | C24H28ClN5O2 |
| 分子量 | 453.96442 |
| EINECS號 | |
| 相關類別 | |
| Mol文件 | 1797983-09-5.mol |
| 結(jié)構(gòu)式 |  |
GSK-J4 鹽酸鹽 性質(zhì)
| 儲存條件 | 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) |
| 形態(tài) | 結(jié)晶固體 |
| 顏色 | 淺黃至黃色 |
| InChIKey | TYXWLTBYINKVNT-UHFFFAOYSA-N |
| SMILES | c1(N2CCc3ccccc3CC2)cc(NCCC(=O)OCC)nc(-c2ncccc2)n1.Cl |
GSK J4 HCl是一種細胞滲透性的GSK J1前體藥物，是第一個選擇性H3K27組蛋白去甲基化酶JMJD3和UTX抑制劑，無細胞試驗中IC50為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胞，抑制脂多糖誘導的細胞因子的產(chǎn)生，包括致炎的腫瘤壞死因子（TNF）。此外，GSK-J4抑制脂多糖誘導的與TNF轉(zhuǎn)錄起始位點相關的H3K27me3損失，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 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
|---|---|---|---|---|---|
| 2026/07/06 | 46800 | GSK-J4 hydrochloride, 95% GSK-J4 hydrochloride, 95% | 1797983-09-5 | 100mg | 8851元 |
| 2026/07/06 | S7070 | GSK-J4 鹽酸鹽 GSK J4 HCl (GSKJ4 HCl) | 1797983-09-5 | 10mg | 1389.07元 |