| 中文名称: | GSK-J4 | ||||
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| 英文名称: | GSK-J4 | ||||
| 别名: | GSK J4 抑制剂;N-[2-(2-吡啶基)-6-(1,2,4,5-四氢-3H-3-苯并氮杂卓-3-基)-4-嘧啶基]-BETA-丙氨酸乙酯;二氯化钨;N-[2-(2-吡啶基)-6-(1,2,4,5-四氢-3H-3-苯并氮杂卓-3-基)-4-嘧啶基]-beta-丙氨酸乙酯 GSK J4;ethyl 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoate;GSK J4 HCl;Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate | ||||
| CAS No: | 1373423-53-0 | 分子式: | C24H27N5O2 | 分子量: | 417.5 |
| CAS No: | 1373423-53-0 | ||||
| 分子式: | C24H27N5O2 | ||||
| 分子量: | 417.5 | ||||
基本信息
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产品编号：G10347 |
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产品名称：GSK-J4 |
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CAS: |
1373423-53-0 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
六个月 |
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分子量： |
417.50 |
-20℃ |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
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Ethanol |
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Water |
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体内（现配现用） |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.3952mL |
11.9760mL |
23.9521mL |
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5mM |
0.4790mL |
2.3952mL |
4.7904mL |
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10mM |
0.2395mL |
1.1976mL |
2.3952mL |
生物活性
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产品描述 |
一种有效的 H3K27me3/me2 去甲基化酶 JMJD3/KDM6B 和 UTX/KDM6A 双抑制剂，IC50 分别为 8.6μM 和 6.6μM。 |
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靶点/IC50 |
8.6µM (JMJD3/KDM6B),6.6µM (UTX/KDM6A) |
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体外研究 |
GSK-J4 has cellular activity in Flag-JMJD3-transfected HeLa cells,in which GSK-J4 prevents the JMJD3-induced loss of nuclear H3K27me3 immunostaining.Administration of GSK-J4 increases total nuclear H3K27me3 levels in untransfected cells.GSK-J4 significantly reduces the expression of 16 of 34 LPS-driven cytokines,including tumour-necrosis factor-α (TNFα).GSK-J4 (5μM;48 hours) causes a more than 3-fold increase in mouse podocyte H3K27me3 content.H3K27me3 levels in cultured podocytes,GSK-J4 reduces Jagged-1 mRNA and Jagged-1 protein levels.Correspondingly,when exposed podocytes to the inducer of dedifferentiation TGF-β1,pretreatment with GSK-J4 preventes both the increase in intracellular N1-ICD levels and the increase in α-SMA and the decrease in podocin mRNA levels.GSK-J4 (10,25nM) acts upon DCs promoting the differentiation of Treg cells, improving Treg stability and suppressive capacities,without affecting the differentiation of Th1 and Th17 cells.GSK-J4 inhibits JMJD3 expression that is induced by TGF-β1.GSK-J4 inhibits H3K4 demethylation at Xist,Nodal,and HoxC13 in female embryonic stem cells. |
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体内研究 |
GSK-J4 Hydrochloride (10mg/kg;i.p.;thrice-weekly for 10 weeks) attenuates the development of kidney disease in diabetic mice.GSK-J4 (0.5mg/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: |
Eight-week-old male db/m and db/db mice |
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Dosage: |
10mg/kg |
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Administration: |
i.p.;thrice-weekly for 10 weeks |
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Result: |
Attenuated the development of kidney disease in diabetic mice. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
