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U0126-EtOH

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U0126-EtOH 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。

貨號(hào)：HY-12031
CAS：1173097-76-1
參數(shù)品牌：MCE
產(chǎn)品參數(shù)
品牌：MCE
型號(hào)：HY-12031
起訂量：1
規(guī)格:：10mg
價(jià)格:：￥750
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產(chǎn)品詳情

U0126-EtOH

U0126-EtOH 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。

生物活性

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


體外研究(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 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[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-G1 phase and to a lesser extent in G2/M[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell 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


體內(nèi)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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:Athymic female nude mice (SWISS, nu/nu)[3].
Dosage:10.5 mg/kg.
Administration:Intraperitoneal injection daily.
Result:Inhibited tumor growth.


分子量：426.56


Formula：C20H22N6OS2


CAS 號(hào)：1173097-76-1


運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.


儲(chǔ)存方式：

Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month


溶解性數(shù)據(jù)

DMSO : 50 mg/mL (117.22 mM; Need ultrasonic)

配制儲(chǔ)備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM2.3443 mL11.7217 mL23.4434 mL
5 mM0.4689 mL2.3443 mL4.6887 mL
10 mM0.2344 mL1.1722 mL2.3443 mL
*

請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 1.


    請(qǐng)依序添加每種溶劑： 0.5% CMC-Na/saline water

    Solubility: 5 mg/mL (11.72 mM); Suspended solution; Need ultrasonic


  • 2.


    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution


  • 3.


    請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution


  • 4.


    請(qǐng)依序添加每種溶劑： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution



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.


U0126-EtOH
U0126-EtOH

U0126-EtOH

分享到微信

×
U0126-EtOH 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。

貨號(hào)：HY-12031
CAS：1173097-76-1
品牌：MCE
型號(hào)：HY-12031
起訂量：1
規(guī)格:：10mg
價(jià)格:：￥750
15906629305
在線客服
產(chǎn)品詳情

U0126-EtOH

U0126-EtOH 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。

生物活性

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


體外研究(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 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[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-G1 phase and to a lesser extent in G2/M[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell 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


體內(nèi)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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:Athymic female nude mice (SWISS, nu/nu)[3].
Dosage:10.5 mg/kg.
Administration:Intraperitoneal injection daily.
Result:Inhibited tumor growth.


分子量：426.56


Formula：C20H22N6OS2


CAS 號(hào)：1173097-76-1


運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.


儲(chǔ)存方式：

Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month


溶解性數(shù)據(jù)

DMSO : 50 mg/mL (117.22 mM; Need ultrasonic)

配制儲(chǔ)備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM2.3443 mL11.7217 mL23.4434 mL
5 mM0.4689 mL2.3443 mL4.6887 mL
10 mM0.2344 mL1.1722 mL2.3443 mL
*

請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 1.


    請(qǐng)依序添加每種溶劑： 0.5% CMC-Na/saline water

    Solubility: 5 mg/mL (11.72 mM); Suspended solution; Need ultrasonic


  • 2.


    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution


  • 3.


    請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution


  • 4.


    請(qǐng)依序添加每種溶劑： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution



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.


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