S81225
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- 公司名稱 上海源葉生物科技有限公司
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- 更新時(shí)間 2024/7/4 7:54:07
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- 產(chǎn)品描述： U0126 (U0126-EtOH) is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC50s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor
- 靶點(diǎn)： MEK2:60 nM (IC50);MEK1:70 nM (IC50)
- 體內(nèi)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
- 參考文獻(xiàn)：
1. Favata MF, et al. Identification of a novel inhibitor of mitogen-activated protein kinase kinase. J Biol Chem. 1998 Jul 17;273(29):18623-32. 2. Droebner K, et al. Antiviral activity of the MEK-inhibitor U0126 against pandemic H1N1v and highly pathogenic avian influenza virus in vitro and in vivo. Antiviral Res. 2011, 92(2), 195-203. 3. Bessard A, et al. RNAi-mediated ERK2 knockdown inhibits growth of tumor cells in vitro and in vivo. Oncogene. 2008 Sep 11;27(40):5315-25. 4. Ahnstedt H, et al. U0126 attenuates cerebral vasoconstriction and improves long-term neurologic outcome after stroke in female rats. J Cereb Blood Flow Metab. 2015 Mar;35(3):454-60.
- 溶解度： DMSO : 50 mg/mL (117.22 mM; Need ultrasonic)
- 保存條件： -20℃
- 配置溶液濃度參考：
1mg 5mg 10mg 1 mM 2.344 ml 11.722 ml 23.443 ml 5 mM 0.469 ml 2.344 ml 4.689 ml 10 mM 0.234 ml 1.172 ml 2.344 ml 50 mM 0.047 ml 0.234 ml 0.469 ml
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