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109511-58-2

中文名稱 1,4-二氨基-2,3-二氰基-1,4-雙(鄰氨基苯巰基)丁二烯
英文名稱 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 結構式 109511-58-2 結構式

基本信息

中文別名
MEK抑制劑(U0126)
1,4-二氨基-2,3-二氰基-1,4-雙(鄰氨基苯硫基)丁二烯
1,4-二氨基-2,3-二氰基-1,4-雙(鄰氨基苯巰基)丁二烯
英文別名
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
所屬類別
生物化工:激動劑抑制劑

物理化學性質

熔點approximate 154℃(dec.)
沸點565.1±50.0 °C(Predicted)
密度1.44
RTECS號EJ9710000
儲存條件Desiccate at +4°C
溶解度溶于DMSO(高達200mg/ml)。
酸度系數(shù)(pKa)2.11±0.10(Predicted)
形態(tài)白色固體
顏色白色
水溶解性Soluble in DMSO. Poorly soluble in ethanol and water
穩(wěn)定性自購買之日起 1 年內保持穩(wěn)定。 DMSO 中的溶液可在 -20° 下保存長達 3 個月。

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335
海關編碼2930909899

常見問題列表

生物活性
U0126 是一種有效,非 ATP 競爭性的,選擇性的 MEK1 和 MEK2 抑制劑,IC50 分別為 72 nM 和 58 nM。U0126-EtOH 是一種自噬 (autophagy) 和線粒體自噬 (mitophagy) 抑制劑。
靶點

MEK2

60 nM (IC 50 )

MEK1

70 nM (IC 50 )

體外研究

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
體內研究

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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