1,4-二氨基-2,3-二氰基-1,4-雙(鄰氨基苯巰基)丁二烯
| 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 |
|---|---|
| 中文同義詞 | 1,4-二氨基-2,3-二氰基-1,4-雙(鄰氨基苯巰基)丁二烯;1,4-二氨基-2,3-二氰基-1,4-雙(鄰氨基苯硫基)丁二烯;MEK抑制劑(U0126);(2Z,3Z)-2,3-雙(氨基((2-氨基苯基)硫代)亞甲基)琥珀腈/U0126;2,3-雙[氨基[(2-氨基苯基)硫代]亞甲基]-丁二腈;U0126,MKK抑制劑;化合物 U0126;U0126,SELECTIVE MKK抑制劑 |
| 英文名稱 | U0126 |
| 英文同義詞 | U0126;1,4-DIAMINO-2,3-DICYANO-1,4-BIS(2-AMINOPHENYLTHIO)BUTADIENE;1,4-DIAMINO-2,3-DICYANO-1,4-BIS(2-AMINOPHYNYLTIO)BUTADIENE;1,4-DIAMINO-2,3-DICYANO-1,4-BIS(O-AMINOPHENYLMERCAPTO)BUTADIENE;1,4-DIAMINO-2,3-DICYANO-1;UO 126;U0126 >99%;2,3-Bis[amino[(2-aminophenyl)thio]methylene]butanedinitrile |
| CAS號 | 109511-58-2 |
| 分子式 | C18H16N6S2 |
| 分子量 | 380.49 |
| EINECS號 | |
| 相關(guān)類別 | 細(xì)胞生物學(xué)試劑;生化試劑;Signalling;Protein Kinase;Inhibitor |
| Mol文件 | 109511-58-2.mol |
| 結(jié)構(gòu)式 | ![]() |
1,4-二氨基-2,3-二氰基-1,4-雙(鄰氨基苯巰基)丁二烯 性質(zhì)
| 熔點(diǎn) | approximate 154℃(dec.) |
|---|---|
| 沸點(diǎn) | 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(dá)200mg/ml)。 |
| 形態(tài) | 白色固體 |
| 酸度系數(shù)(pKa) | 2.11±0.10(Predicted) |
| 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(nèi)保持穩(wěn)定。 DMSO 中的溶液可在 -20° 下保存長達(dá) 3 個(gè)月。 |
| InChI | 1S/C18H16N6S2/c19-9-11(17(23)25-15-7-3-1-5-13(15)21)12(10-20)18(24)26-16-8-4-2-6-14(16)22/h1-8H,21-24H2/b17-11+,18-12+ |
| InChIKey | DVEXZJFMOKTQEZ-JYFOCSDGSA-N |
| SMILES | S(c2c(cccc2)N)\C(=C(\C(=C(\Sc1c(cccc1)N)/N)\C#N)/C#N)\N |
|
MEK2 60 nM (IC 50 ) |
MEK1 70 nM (IC 50 ) |
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 |
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. |
安全信息
| WGK Germany | WGK 1 |
|---|---|
| 海關(guān)編碼 | 2930909899 |
| 存儲類別 | 10 - 可燃性液體 |
| 更新日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價(jià)格 |
|---|---|---|---|---|---|
| 2026/06/05 | HY-12031A | 1,4-二氨基-2,3-二氰基-1,4-雙(鄰氨基苯巰基)丁二烯 U0126 | 109511-58-2 | 5 mg | 1200元 |
| 2026/06/05 | HY-12031A | 1,4-二氨基-2,3-二氰基-1,4-雙(鄰氨基苯巰基)丁二烯 U0126 | 109511-58-2 | 10 mM * 1 mLin DMSO | 1320元 |
