1. PI3K/Akt/mTOR Autophagy
  2. mTOR Autophagy
  3. MHY1485

MHY1485 is a potent cell-permeable mTOR activator that targets the ATP domain of mTOR. MHY1485 inhibits autophagy by suppression of fusion between autophagosomes and lysosomes.

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CAS 番号 : 326914-06-1

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 60 在庫あり
Solution
10 mM * 1 mL in DMSO USD 60 在庫あり
Solid
5 mg $55 在庫あり
10 mg $77 在庫あり
25 mg $150 在庫あり
50 mg $242 在庫あり
100 mg $440 在庫あり
200 mg $770 在庫あり
500 mg $1300 在庫あり
1 g $1950 在庫あり
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カスタマーレビュー

Based on 201 publication(s) in Google Scholar

Top Publications Citing Use of Products

顧客検証

WB

    MHY1485 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2019 Feb 13;10(2):140.   [Abstract]

    Sorted naive T cells are cultured with TGF-β, IL-2 with or without 40 μM Baicalin or 10 μM MHY1485 for 3 h, P-mTOR, p-S6K, P-4EBP1, and GAPDH expression are analyzed by western blot.

    MHY1485 purchased from MedChemExpress. Usage Cited in: Neurochem Res. 2018 Nov;43(11):2141-2154.  [Abstract]

    MHY1485 (M) increases phospho-mTOR (Ser 2448), phosphoS6K1 (Thr 389) and NGF expression in RSC96 cells.

    MHY1485 purchased from MedChemExpress. Usage Cited in: Exp Cell Res. 2018 Jun 15;367(2):186-195.  [Abstract]

    MHY1485 prevents high glucose-caused reduced phospho-S6K1 (Thr 389) and cell apoptosis in RSC96 cells.

    MHY1485 purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2018 Jul;119(7):6104-6112.  [Abstract]

    MHY-1485 significantly suppresses the increase in LC3II/LC3I ratios induced by Cucurbitacin I.

    MHY1485 purchased from MedChemExpress. Usage Cited in: Exp Cell Res. 2017 Nov 15;360(2):328-336.  [Abstract]

    HT29 cells are co-treated with 5-FU and MHY1485 (MHY) for 48 h. Proteins are collected and immunoblotted with mTOR, p-p70S6K, and p70S6K, with β-actin as the loading control.

    MHY1485 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Feb 21;8(8):12775-12783.  [Abstract]

    OSI-027, AZD-8055 and AZD-2014 almost completely block MHY1485-induced mTOR activation (p-mTOR/S6K1/Akt Ser473) in skin keratinocytes.

    MHY1485 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2016 Dec 15:122:42-61.  [Abstract]

    Inhibition of SREBPs processing by AHI is dependent on LKB-1/AMPK/mTOR pathway. (A) HepG2 cells are incubated with or without MHY1485 or Rapamycin for 1 h, the cells are switched to medium D in the presence of vehicle, or AHI. (B) HepG2 cells are incubated with or without Compound C for 1 h, the cells are switched to medium D in the presence of vehicle, or AHI.

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    製品説明

    MHY1485 is a potent cell-permeable mTOR activator that targets the ATP domain of mTOR. MHY1485 inhibits autophagy by suppression of fusion between autophagosomes and lysosomes[1].

    IC50 & Target[4]

    mTORC1

     

    mTORC2

     

    Autophagy

     

    体外実験

    MHY1485 (10 μM; 4 hours) shows that GCDC-induced autophagic activity is inhibited by upregulating p-mTOR expression and downregulating LC3 and p62 expression in HCC cells[1].
    MHY1485 (5 μM; 6 hours) increases the LC3II/LC3I ratio in a dose and time-dependently manner due to presumably inhibited LC3II degradation in rat liver Ac2F cells[2].
    MHY1485 (0.5-2 μM; 6 hours) increases the phosphorylation of mTOR at ser2448 and upregulates the level of phosphorylation of 4E-BP1 in a dose-dependently manner in Ac2F cells[2].

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

    Western Blot Analysis[1]

    Cell Line: HCC cells
    Concentration: 10 μM
    Incubation Time: 4 hours
    Result: Upregulated p-mTOR and downregulated LC3 and p62 expression.
    体内実験

    MHY1485 (intraperitoneal injection; 10?mg/kg, 2 days) blocks the autophagy signaling induced by follicle-stimulating hormone (FSH). It increases p-mTOR and p-S6K1 expression levels, whereas LC3 expression shows no marked change compared to that in the control group[3].

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

    Animal Model: 4-week-old female ICR mice[3]
    Dosage: 10 mg/kg, 2 days
    Administration: Intraperitoneal injection
    Result: Suppressed the autophagy level following FSH treatment. 
    分子量

    387.39

    分子式

    C17H21N7O4

    CAS 番号
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    O=[N+](C1=CC=C(NC2=NC(N3CCOCC3)=NC(N4CCOCC4)=N2)C=C1)[O-]

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 7 mg/mL (18.07 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : < 1 mg/mL (insoluble)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5814 mL 12.9069 mL 25.8138 mL
    5 mM 0.5163 mL 2.5814 mL 5.1628 mL
    10 mM 0.2581 mL 1.2907 mL 2.5814 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 0.77 mg/mL (1.99 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.77 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 0.77 mg/mL (1.99 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.77 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.7 mg/mL) to 900 μL Corn oil, and mix evenly.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 1.67 mg/mL (4.31 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  20% HP-β-CD in Saline

      Solubility: 1 mg/mL (2.58 mM); Suspended solution; Need ultrasonic

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    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.93%

    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5814 mL 12.9069 mL 25.8138 mL 64.5344 mL
    5 mM 0.5163 mL 2.5814 mL 5.1628 mL 12.9069 mL
    10 mM 0.2581 mL 1.2907 mL 2.5814 mL 6.4534 mL
    15 mM 0.1721 mL 0.8605 mL 1.7209 mL 4.3023 mL
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    一般には略語で表示されます:C1V1 = C2V2

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    製品名:
    MHY1485
    製品番号:
    HY-B0795
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