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

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;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-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)prop;Histone Lysine Demethylase Inhibitor VIII, GSK-J4
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;Inhibitor;Inhibitors;API
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 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

沸点581.2±50.0 °C(Predicted)
密度1.216±0.06 g/cm3(Predicted)
储存条件2-8°C
溶解度在DMSO中的溶解度为20mg/mL,澄清
酸度系数(pKa)5.95±0.10(Predicted)
形态棕褐色半固体状
颜色白色至米色
稳定性可在-20°下的DMSO或乙醇溶液保存长达3个月。
InChIKeyWBKCKEHGXNWYMO-UHFFFAOYSA-N

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

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)。

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

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.

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.

Animal Model: Eight-week-old male db/m and db/db mice
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

危险品标志Xi
危险类别码36/37/38
安全说明26
WGK Germany3

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/01/25HY-15648BGSK-J45 mg750元
2024/01/25HY-15648BN-[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
1373423-53-010mg1200元

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

"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"相关产品信息
2-氰基吡啶 GSK2982772 GSK2636771 GSK3685032 FREEBASE N-(6-氟-1H-吲唑-5-基)-2-甲基-6-氧代-4-[4-(三氟甲基)苯基]-1,4,5,6-四氢-3-吡啶甲酰胺 曲古柳菌素A 白藜芦醇 RVX-208 5-氮杂胞苷 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 N-[2-(3-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 N-[2-(3-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 BIX01294 GSK343 5-氯-2(1H)-吡啶酮(2E)-(苯基-2-吡啶基亚甲基)腙 EPZ5676 OG-L002
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