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Wortmannin (渥曼青霉素)

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Wortmannin (SL-2052) 是一種有效的,不可逆的,選擇性PI3K 抑制劑,IC50 值為 3 nM。Wortmannin (SL-2052) 阻斷自噬 (autophagy) 形成,并有效抑制 Polo-like kinase 1 (PlK1) 和 Plk3,IC50 值分別為 5.8 和 48 nM。

貨號:HY-10197
CAS:19545-26-7
參數(shù)品牌:MCE
產品參數(shù)
品牌:MCE
型號:HY-10197
起訂量:1
規(guī)格::5mg
價格::¥800
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產品詳情

Wortmannin (Synonyms: 渥曼青霉素)

Wortmannin (SL-2052) 是一種有效的,不可逆的,選擇性PI3K 抑制劑,IC50 值為 3 nM。Wortmannin (SL-2052) 阻斷自噬 (autophagy) 形成,并有效抑制 Polo-like kinase 1 (PlK1) 和 Plk3IC50 值分別為 5.8 和 48 nM。

生物活性

Wortmannin (SL-2052; KY-12420) is a potent, selective and irreversible PI3K inhibitor with an IC50 of 3 nM. Wortmannin also blocks autophagy formation, and potently inhibits Polo-like kinase 1 (PlK1) and Plk3 with IC50s of 5.8 and 48 nM, respectively[1][2][3].


體外研究(In Vitro)

Wortmannin (0-100 nM; 24-72 hours) inhibits the proliferation of K562 cells in a time- and dose-dependent manner. The IC50 values at 24 hour, 48 hour, and 72 hour are 25±0.10 nM, 12.5±0.08 nM, and 6.25±0.11 nM, respectively[4]. Wortmannin prevents nuclear entry of YAP[6].

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

Cell Proliferation Assay[4]

Cell Line:K562 cells
Concentration:0, 6.25, 12.5, 25, 50 and 100 nM
Incubation Time:0, 24, 48 and 72 hours
Result:Inhibited the K562 cells proliferation. The IC50 value at 24 hour, 48 hour, and 72 hour was 25±0.10 nM, 12.5±0.08 nM, and 6.25±0.11 nM.


體內研究(In Vivo)

Wortmannin (oral gavage; daily; in Scid mice; one group of eight mice is dosed with Wortmannin 1 mg/kg for all 14 days. The second group of eight mice is dosed with Wortmannin 1.5 mg/kg for the first 5 days and the dose is decreased to 1 mg/kg for the remaining treatment period) treatment significantly slower the growth rate of murine C3H mammary tumor and human MCF-7 breast cancer xenograft. A dose of 1 mg/kg Wortmannin for 7 days decrease the tumor burdens in mice with established murine C3H mammary tumors by 54% relative to controls. Human MCF-7 breast cancer xenograft burdens are decreased by 97% relative to controls after 14 days of 1 mg/kg Wortmannin beginning 1 day after tumor implantation[5].

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

Animal Model:Scid mice with the murine C3H mammary tumor or human MCF-7 breast cancer xenograft[5]
Dosage:1 mg/kg and 1.5 mg/kg
Administration:Oral gavage; daily; one group 1 mg/kg for 14 days; second group 1.5 mg/kg for 5 days then 1.0 mg/kg for 9 days.
Result:The growth rate of the treated tumors was significantly slower during drug administration than that of nontreated tumors.


分子量:428.43


Formula:C23H24O8


CAS 號:19545-26-7


中文名稱:渥曼青霉素;沃氏籃酶素;奧特曼寧


運輸條件:Room temperature in continental US; may vary elsewhere.


儲存方式

Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month


溶解性數(shù)據(jù)


In Vitro: 

DMSO : ≥ 50 mg/mL (116.71 mM)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度溶劑體積質量1 mg5 mg10 mg
1 mM2.3341 mL11.6705 mL23.3410 mL
5 mM0.4668 mL2.3341 mL4.6682 mL
10 mM0.2334 mL1.1671 mL2.3341 mL
*

請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產品失效
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲存時,請在 6 個月內使用,-20°C 儲存時,請在 1 個月內使用。

In Vivo:

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

——為保證實驗結果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用; 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.


    請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.08 mg/mL (4.85 mM); Suspended solution; Need ultrasonic


  • 2.


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

    Solubility: ≥ 2.08 mg/mL (4.85 mM); Clear solution


  • 3.


    請依序添加每種溶劑: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.85 mM); Clear solution


參考文獻

[1]. Yano H, et al. Inhibition of histamine secretion by wortmannin through the blockade of phosphatidylinositol 3-kinase in RBL-2H3 cells. J Biol Chem. 1993 Dec 5;268(34):25846-56.

[2]. Moon EK, et al. Autophagy inhibitors as a potential antiamoebic treatment for Acanthamoeba keratitis. Antimicrob Agents Chemother. 2015 Jul;59(7):4020-5.

[3]. Liu Y, et al. Polo-like kinases inhibited by wortmannin. Labeling site and downstream effects. J Biol Chem. 2007 Jan 26;282(4):2505-11.

[4]. Wu Q, et al. Wortmannin inhibits K562 leukemic cells by regulating PI3k/Akt channel in vitro. J Huazhong Univ Sci Technolog Med Sci. 2009 Aug;29(4):451-6.

[5]. Lemke LE, et al. Wortmannin inhibits the growth of mammary tumors despite the existence of a novel wortmannin-insensitive phosphatidylinositol-3-kinase. Cancer Chemother Pharmacol. 1999;44(6):491-7.

[6]. Liu Y, et al. Wortmannin, a widely used phosphoinositide 3-kinase inhibitor, also potently inhibits mammalianpolo-like kinase. Chem Biol. 2005 Jan;12(1):99-107.

[7]. Pobbati AV, et al. A combat with the YAP/TAZ-TEAD oncoproteins for cancer therapy. Theranostics. 2020 Feb 18;10(8):3622-3635.






Wortmannin (渥曼青霉素)
Wortmannin (渥曼青霉素)

Wortmannin (渥曼青霉素)

分享到微信

×
Wortmannin (SL-2052) 是一種有效的,不可逆的,選擇性PI3K 抑制劑,IC50 值為 3 nM。Wortmannin (SL-2052) 阻斷自噬 (autophagy) 形成,并有效抑制 Polo-like kinase 1 (PlK1) 和 Plk3,IC50 值分別為 5.8 和 48 nM。

貨號:HY-10197
CAS:19545-26-7
品牌:MCE
型號:HY-10197
起訂量:1
規(guī)格::5mg
價格::¥800
15906629305
在線客服
產品詳情

Wortmannin (Synonyms: 渥曼青霉素)

Wortmannin (SL-2052) 是一種有效的,不可逆的,選擇性PI3K 抑制劑,IC50 值為 3 nM。Wortmannin (SL-2052) 阻斷自噬 (autophagy) 形成,并有效抑制 Polo-like kinase 1 (PlK1) 和 Plk3,IC50 值分別為 5.8 和 48 nM。

生物活性

Wortmannin (SL-2052; KY-12420) is a potent, selective and irreversible PI3K inhibitor with an IC50 of 3 nM. Wortmannin also blocks autophagy formation, and potently inhibits Polo-like kinase 1 (PlK1) and Plk3 with IC50s of 5.8 and 48 nM, respectively[1][2][3].


體外研究(In Vitro)

Wortmannin (0-100 nM; 24-72 hours) inhibits the proliferation of K562 cells in a time- and dose-dependent manner. The IC50 values at 24 hour, 48 hour, and 72 hour are 25±0.10 nM, 12.5±0.08 nM, and 6.25±0.11 nM, respectively[4]. Wortmannin prevents nuclear entry of YAP[6].

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

Cell Proliferation Assay[4]

Cell Line:K562 cells
Concentration:0, 6.25, 12.5, 25, 50 and 100 nM
Incubation Time:0, 24, 48 and 72 hours
Result:Inhibited the K562 cells proliferation. The IC50 value at 24 hour, 48 hour, and 72 hour was 25±0.10 nM, 12.5±0.08 nM, and 6.25±0.11 nM.


體內研究(In Vivo)

Wortmannin (oral gavage; daily; in Scid mice; one group of eight mice is dosed with Wortmannin 1 mg/kg for all 14 days. The second group of eight mice is dosed with Wortmannin 1.5 mg/kg for the first 5 days and the dose is decreased to 1 mg/kg for the remaining treatment period) treatment significantly slower the growth rate of murine C3H mammary tumor and human MCF-7 breast cancer xenograft. A dose of 1 mg/kg Wortmannin for 7 days decrease the tumor burdens in mice with established murine C3H mammary tumors by 54% relative to controls. Human MCF-7 breast cancer xenograft burdens are decreased by 97% relative to controls after 14 days of 1 mg/kg Wortmannin beginning 1 day after tumor implantation[5].

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

Animal Model:Scid mice with the murine C3H mammary tumor or human MCF-7 breast cancer xenograft[5]
Dosage:1 mg/kg and 1.5 mg/kg
Administration:Oral gavage; daily; one group 1 mg/kg for 14 days; second group 1.5 mg/kg for 5 days then 1.0 mg/kg for 9 days.
Result:The growth rate of the treated tumors was significantly slower during drug administration than that of nontreated tumors.


分子量:428.43


Formula:C23H24O8


CAS 號:19545-26-7


中文名稱:渥曼青霉素;沃氏籃酶素;奧特曼寧


運輸條件:Room temperature in continental US; may vary elsewhere.


儲存方式

Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month


溶解性數(shù)據(jù)


In Vitro: 

DMSO : ≥ 50 mg/mL (116.71 mM)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度溶劑體積質量1 mg5 mg10 mg
1 mM2.3341 mL11.6705 mL23.3410 mL
5 mM0.4668 mL2.3341 mL4.6682 mL
10 mM0.2334 mL1.1671 mL2.3341 mL
*

請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲存時,請在 6 個月內使用,-20°C 儲存時,請在 1 個月內使用。

In Vivo:

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

——為保證實驗結果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用; 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.


    請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.08 mg/mL (4.85 mM); Suspended solution; Need ultrasonic


  • 2.


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

    Solubility: ≥ 2.08 mg/mL (4.85 mM); Clear solution


  • 3.


    請依序添加每種溶劑: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.85 mM); Clear solution


參考文獻

[1]. Yano H, et al. Inhibition of histamine secretion by wortmannin through the blockade of phosphatidylinositol 3-kinase in RBL-2H3 cells. J Biol Chem. 1993 Dec 5;268(34):25846-56.

[2]. Moon EK, et al. Autophagy inhibitors as a potential antiamoebic treatment for Acanthamoeba keratitis. Antimicrob Agents Chemother. 2015 Jul;59(7):4020-5.

[3]. Liu Y, et al. Polo-like kinases inhibited by wortmannin. Labeling site and downstream effects. J Biol Chem. 2007 Jan 26;282(4):2505-11.

[4]. Wu Q, et al. Wortmannin inhibits K562 leukemic cells by regulating PI3k/Akt channel in vitro. J Huazhong Univ Sci Technolog Med Sci. 2009 Aug;29(4):451-6.

[5]. Lemke LE, et al. Wortmannin inhibits the growth of mammary tumors despite the existence of a novel wortmannin-insensitive phosphatidylinositol-3-kinase. Cancer Chemother Pharmacol. 1999;44(6):491-7.

[6]. Liu Y, et al. Wortmannin, a widely used phosphoinositide 3-kinase inhibitor, also potently inhibits mammalianpolo-like kinase. Chem Biol. 2005 Jan;12(1):99-107.

[7]. Pobbati AV, et al. A combat with the YAP/TAZ-TEAD oncoproteins for cancer therapy. Theranostics. 2020 Feb 18;10(8):3622-3635.






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