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号:1373423-53-0
- 英文名:GSK J4 HCl
- 中文名: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
- CBNumber:CB62665155
- 分子式:C24H27N5O2
- 分子量:417.5
- MOL File:1373423-53-0.mol
- 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 :DMSO: soluble20mg/mL, clear
- 酸度系数(pKa) :5.95±0.10(Predicted)
- 形态 :Tan semi-solid
- 颜色 :white to beige
- 稳定性 :Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
- InChIKey :WBKCKEHGXNWYMO-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-丙氨酸乙酯性质、用途与生产工艺
- 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.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.
- 更新日期:2024/11/08
- 产品编号:HY-15648B
- 产品名称:GSK-J4
- CAS编号:
- 包装:5 mg
- 价格:750元
- 更新日期:2024/11/08
- 产品编号:HY-15648B
- 产品名称: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 GSK-J4
- CAS编号:1373423-53-0
- 包装:10mg
- 价格:1195元
- 公司名称:济南精合医药科技有限公司
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- 2-氰基吡啶 GSK2982772 GSK2636771 GSK 3685032 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 BIX 01294 GSK343 5-氯-2(1H)-吡啶酮 (2E)-(苯基-2-吡啶基亚甲基)腙 EPZ 5676 OG-L002