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109511-58-2

中文名称 1,4-二氨基-2,3-二氰基-1,4-双(邻氨基苯巯基)丁二烯
英文名称 U0126
CAS 109511-58-2
分子式 C18H16N6S2
分子量 380.49
MOL 文件 109511-58-2.mol
更新日期 2024/05/20 09:19:55
109511-58-2 结构式 109511-58-2 结构式

基本信息

中文别名
MEK抑制剂(U0126)
1,4-二氨基-2,3-二氰基-1,4-双(邻氨基苯硫基)丁二烯
1,4-二氨基-2,3-二氰基-1,4-双(邻氨基苯巯基)丁二烯
英文别名
U0126
UO 126
CS-1122
U0126 >99%
U0126, >=98%
U0126
U 0126
U0126 (Uo126)
U 0126 - U 126
1,4-DIAMINO-2,3-DICYANO-1
Bis[amino(o-aminophenylthio)methylene]succinonitrile
所属类别
生物化工:激动剂抑制剂

物理化学性质

熔点approximate 154℃(dec.)
沸点565.1±50.0 °C(Predicted)
密度1.44
RTECS号EJ9710000
储存条件Desiccate at +4°C
溶解度溶于DMSO(高达200mg/ml)。
酸度系数(pKa)2.11±0.10(Predicted)
形态白色固体
颜色白色
水溶解性Soluble in DMSO. Poorly soluble in ethanol and water
稳定性自购买之日起 1 年内保持稳定。 DMSO 中的溶液可在 -20° 下保存长达 3 个月。

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H302-H315-H319-H335
海关编码2930909899

常见问题列表

生物活性
U0126 是一种有效,非 ATP 竞争性的,选择性的 MEK1 和 MEK2 抑制剂,IC50 分别为 72 nM 和 58 nM。U0126-EtOH 是一种自噬 (autophagy) 和线粒体自噬 (mitophagy) 抑制剂。
靶点

MEK2

60 nM (IC 50 )

MEK1

70 nM (IC 50 )

体外研究

Treatment with U0126 efficiently reduces progeny virus titers of all tested strains in A549 cells. While nM concentrations of U0126 are efficient to reduce H1N1v and H5N1 (MB1), μM concentrations of U0126 are required to reduce the virus titer of H5N1 (GSB) and H7N7. The EC 50 values for U0126-EtOH against H1N1v are 1.2±0.4 μM in A549 cells and 74.7±1.0 μM in MDCKII cells.
Rat hepatocarcinoma cells (FAO) stimulated by fetal calf serum (FCS) exhibits a significant proportion in S phase (32.62%) whereas U0126 strongly decreases the proportion of cells in S phase (9.92%) and increases the proportion of cells in G 0 -G 1 phase and to a lesser extent in G 2 /M.

Cell Viability Assay

Cell Line: A549 and MDCK II cells.
Concentration: 0.001-1000 μM.
Incubation Time: 48 h.
Result: The EC 50 values for U0126 against H1N1v were 1.2 ± 0.4 μM in A549 cells and 74.7 ± 1.0 μM in MDCKII cells
体内研究

Mice are treated daily with U0126-EtOH (U0126; i.p., 10.5 mg/kg). In control experiment, tumor sizes are constant or slightly increase all over the kinetic. At the opposite, in all U0126-EtOH experiments, engraftment and early tumor growth are significantly decreased. Furthermore, a 60-70% reduction in the volume of tumors treated with U0126-EtOH is obtained 9 days after injection and thereafter.
Rats are subjected to 120 minutes transient middle cerebral artery occlusion (tMCAO) and thereafter treated with the U0126-EtOH (U0126; i.p., 30 mg/kg) at 0 and 24 hours of reperfusion. After treatment with U0126-EtOH, the vasoconstriction to S6c is markedly reduced.

Animal Model: Athymic female nude mice (SWISS, nu/nu).
Dosage: 10.5 mg/kg.
Administration: Intraperitoneal injection daily.
Result: Inhibited tumor growth.
Animal Model: Twelve-week-old female Wistar rats (250 to 265 g) .
Dosage: 30 mg/kg.
Administration: Intraperitoneally.
Result: The vasoconstriction to S6c is markedly reduced.
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