U0126-EtOH

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

U0126 (U0126-EtOH) 是一种有效的选择性 MEK (MAP2K) 抑制剂，对于 MEK1 和 MEK2 的 IC50 分别为 70 nM 和 60 nM。

U0126 (U0126-EtOH) is a potent, selective MEK (MAP2K) inhibitor with IC50 of 70 nM and 60 nM for MEK1 and MEK2, suppresses AP-1-mediated gene activation in transient transfection assays with IC50 of 0.96 uM; shows little to no effect on the kinase activities of PKC, Abl, Raf, MEKK, ERK, JNK, MKK-3, MKK-4/SEK, MKK-6, Cdk2, or Cdk4; inhibits T cell proliferation in response to antigenic stimulation or cross-linked anti-CD3 plus anti-CD28 Abs, but has no effect on IL-2-induced proliferation; reduces tumor size of tumor xenografts in nude mice.(In Vitro):Treatment with U0126-EtOH (U0126) efficiently reduces progeny virus titers of all tested strains in A549 cells. While nM concentrations of U0126-EtOH are efficient to reduce H1N1v and H5N1 (MB1), μM concentrations of U0126-EtOH are required to reduce the virus titer of H5N1 (GSB) and H7N7. The EC50 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-EtOH (U0126) strongly decreases the proportion of cells in S phase (9.92%) and increases the proportion of cells in G0-G1 phase and to a lesser extent in G2/M.(In Vivo):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.

Treatment with U0126-EtOH (U0126) efficiently reduces progeny virus titers of all tested strains in A549 cells. While nM concentrations of U0126-EtOH are efficient to reduce H1N1v and H5N1 (MB1), μM concentrations of U0126-EtOH are required to reduce the virus titer of H5N1 (GSB) and H7N7. The EC50 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-EtOH (U0126) strongly decreases the proportion of cells in S phase (9.92%) and increases the proportion of cells in G0-G1 phase and to a lesser extent in G2/M. Cell Viability AssayCell Line:A549 and MDCK II cells.Concentration:0.001-1000 μM.Incubation Time:48 h.Result:The EC50 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.

U0126-EtOH | U 0126 | U-0126

MAPK/ERK Signaling

MEK

CDK2|CDK4|MEK1|MEK2|PKC

Cancer

——

1173097-76-1

426.5583

C20H22N6OS2

>98% (HPLC)

DMSO: ≥ 49 mg/mL

CCO.C1=CC=C(C(=C1)N)SC(=C(C#N)C(=C(N)SC2=CC=CC=C2N)C#N)N

Butanedinitrile, 2,3-bis[amino[(2-aminophenyl)thio]methylene]-, compd. with ethanol (1:1)

(-20℃)

With Ice Pack

≥ 2 years