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 CAS#: 1373423-53-0

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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

生物活性靶点体外研究体内研究 用途与合成方法 MSDS 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-丙氨酸乙酯价格(试剂级) 上下游产品信息

中文名称	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
中文同义词	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 游离(检测J4溶样不要用甲醇,会发生酯交换);H3K27ME3DEMETHYLASE抑制剂(GSK-J4);1373423-53-0 的盐酸盐;6-三碘苯酚;3-((6-(4,5-二氢-1H-苯并[D]氮杂卓-3(2H)-基)-2-(吡啶-2-基)嘧啶-4-基)氨基)丙酸乙酯;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;GSK-J4,细组蛋白脱甲基酶JMJD3 / UTX抑制剂
英文名称	GSK J4 HCl
英文同义词	GSK J4;GSK-J4;N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-beta-alanine ethyl ester;GSK J4 HCl;N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyriMidinyl]-|-alanine ethyl ester;β-Alanine, N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-, ethyl ester, hydrochloride (1:1);Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate;ethyl 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoate
CAS号	1373423-53-0
分子式	C24H27N5O2
分子量	417.5
EINECS号
相关类别	小分子抑制剂，天然产物;活性分子;细胞生物学试剂;API;Inhibitor;Inhibitors
Mol文件	1373423-53-0.mol
结构式

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 性质

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 用途与合成方法

生物活性

GSK-J4 是一种有效的 H3K27me3/me2 去甲基化酶 JMJD3/KDM6B 和 UTX/KDM6A 双抑制剂，IC50 分别为 8.6 μM 和 6.6 μM。GSK-J4 抑制 LPS 诱导的人原代巨噬细胞产生 TNF-α，IC50 值为 9 μM。GSK-J4 是 GSK-J1 的细胞通透性前药。GSK-J4 诱导内质网应激相关的细胞凋亡 (apoptosis)。

靶点

IC50: 8.6 µM (JMJD3/KDM6B), 6.6 µM (UTX/KDM6A)

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 (TNF-α).  
 GSK-J4 (5 μM; 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, 25 nM) 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.

体内研究

GSK-J4 Hydrochloride (10 mg/kg; i.p.; thrice-weekly for 10 weeks) attenuates the development of kidney disease in diabetic mice.  
 GSK-J4 (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.

安全信息

MSDS信息

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 价格(试剂级)

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 上下游产品信息

上游原料

4,6-二氯-2-[2-吡啶]嘧啶2,3,4,5 -四氢-1H -苯并[D]氮杂卓