U0126-EtOH 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。
生物活性 | U0126 (U0126-EtOH) is a potent, non-ATP competitive and selectiveMEK1andMEK2inhibitor, withIC50s of 72 nM and 58 nM, respectively. U0126 is anautophagyandmitophagyinhibitor[1][2][3][4]. |
IC50& Target[1] | MEK2 60 nM (IC50) | MEK1 70 nM (IC50) |
|
体外研究 (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 EC50values for U0126-EtOH against H1N1v are 1.2±0.4 μM in A549 cells and 74.7±1.0 μM in MDCKII cells[2]. 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-G1phase and to a lesser extent in G2/M[3].
Cell Viability Assay[2] Cell Line: | A549 and MDCK II cells. | Concentration: | 0.001-1000 μM. | Incubation Time: | 48 h. | Result: | The EC50values 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 (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[3]. 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[4].
Animal Model: | Athymic female nude mice (SWISS, nu/nu)[3]. | 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)[4]. | Dosage: | 30 mg/kg. | Administration: | Intraperitoneally. | Result: | The vasoconstriction to S6c is markedly reduced. |
|
分子量 | |
性状 | |
Formula | |
CAS 号 | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
溶解性数据 | In Vitro: DMSO : 50 mg/mL(117.22 mM;Need ultrasonic) 配制储备液 1 mM | 2.3443 mL | 11.7217 mL | 23.4434 mL | 5 mM | 0.4689 mL | 2.3443 mL | 4.6887 mL | 10 mM | 0.2344 mL | 1.1722 mL | 2.3443 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 0.5%CMC-Na/saline water Solubility: 5 mg/mL (11.72 mM); Suspended solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.88 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.88 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 4. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.88 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
|