2. Apoptosis Autophagy
  3. c-Myc Autophagy
  4. 10058-F4

10058-F4 is a c-Myc inhibitor that prevents c-Myc-Max dimerization and transactivation of c-Myc target gene expression.

For research use only. We do not sell to patients.

10058-F4 Chemical Structure

10058-F4 Chemical Structure

CAS No. : 403811-55-2

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Customer Review

Based on 40 publication(s) in Google Scholar

10058-F4 Related Antibodies

Top Publications Citing Use of Products

38 Publications Citing Use of MCE 10058-F4

WB

    10058-F4 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Feb 22;9(3):307.  [Abstract]

    ACHN cells are treated with or without 10058-F4 for 24 h. After the 24-h treatment, proteins are extracted. Immunoblotting assays are performed to analyse E-cadherin, N-cadherin, Vimentin, ZEB1, ZEB2, Snail1, Snail2, Twist, Smad2, Smad3, p-Smad2 and p-Smad3 protein levels. GAPDH is used as the loading control.

    10058-F4 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Feb 22;9(3):307.  [Abstract]

    786-O cells are treated with or without 10058-F4 for 24 h. After the 24-h treatment, proteins are extracted. Immunoblotting assays are performed to analyse E-cadherin, N-cadherin, Vimentin, ZEB1, ZEB2, Snail1, Snail2 , Twist, Smad2, Smad3, p-Smad2 and p-Smad3 protein levels. GAPDH is used as the loading control.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    10058-F4 is a c-Myc inhibitor that prevents c-Myc-Max dimerization and transactivation of c-Myc target gene expression.

    In Vitro

    10058-F4 inhibits growth of leukemic cells and dimerization of Myc and Max. 10058-F4 induces cell-cycle arrest and apoptosis of AML cells. 10058-F4 arrests AML cells at G0/G1 phase, downregulates c-Myc expression and upregulated CDK inhibitors, p21 and p27. Meanwhile, 10058-F4 induces apoptosis through activation of mitochondrial pathway shown by downregulation of Bcl-2, upregulation of Bax, release of cytoplasmic cytochrome C, and cleavage of caspase 3, 7, and 9. Furthermore, 10058-F4 also induces myeloid differentiation, possibly through activation of multiple transcription factors. Similarly, 10058-F4-induced apoptosis and differentiation could also be observed in primary AML cells[1].
    10058-F4 decreases c-Myc protein levels, inhibites proliferation of HepG2 cells likely through upregulation of cyclin-dependent kinase (cdk) inhibitor, p21WAF1 and lowers intracellular levels of [alpha]-fetoprotein (AFP). Treatment with 10058-F4 also downregulates human telomerase reverse transcriptase (hTERT) at the transcriptional level. In addition to inhibiting the proliferation of HepG2 cells, 10058-F4 enhances sensitivity to conventional chemotherapeutic agents, doxorubicin, 5-fluorouracil (5-FU) and cisplatin[2].

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

    10058-F4 Related Antibodies
    In Vivo

    Peak plasma 10058-F4 concentrations of approximately 300 μM are seen at 5 min and declined to below the detection limit at 360 min following a single iv dose. Plasma concentration versus time data are best approximated by a two-compartment, open, linear model. The highest tissue concentrations of 10058-F4 are found in fat, lung, liver, and kidney. Peak tumor concentrations of 10058-F4 are at least tenfold lower than peak plasma concentrations. Eight metabolites of 10058-F4 are identified in plasma, liver, and kidney. The terminal half-life of 10058-F4 is approximately 1 h, and the volume of distribution is > 200 mL/kg. No significant inhibition of tumor growth is seen after i.v. treatment of mice with either 20 or 30 mg/kg 10058-F4[3].

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

    249.35

    Formula

    C12H11NOS2
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C1NC(S/C1=C/C2=CC=C(CC)C=C2)=S
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 41 mg/mL (164.43 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.0104 mL 20.0521 mL 40.1043 mL
    5 mM 0.8021 mL 4.0104 mL 8.0209 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    Volume (final)

    V2

    In Vivo:

    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: ≥ 0.83 mg/mL (3.33 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 0.83 mg/mL (3.33 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    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.
    Purity & Documentation

    Purity: 99.77%

    COA (247 KB) LCMS (267 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    Cells, plated in 96-well plates (105/mL for cell lines and 5×105/mL for primary leukemic cells), are treated in triplicate with indicated concentrations of 10058-F4. At various time points, 20 μL 5 mg/mL MTT is added to each well. After incubation at 37°C for 3 hours, the MTT medium is removed and 100 μL DMSO lysis buffer is added. The number of viable cells is assessed by the percentage of absorbance of treated cells relative to that of solvent controls, using 570-nm wavelength on a spectrophotometer.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    C B-17 SCID mice bearing PC-3 human prostate tumor xenografts are stratified into the following groups: Control, vehicle control, positive control (docetaxel, 10 mg/kg), and 10058-F4 treatment (20 or 30 mg/kg/dose). Previous studies by us indicates that 30 mg/kg is the maximally tolerated dose of 10058-F4 on this schedule. Mice are treated i.v. daily for 5 days for 2 weeks, and body weights and tumor volumes are recorded twice weekly. In the second study, C B-17 SCID mice bearing DU145 human androgen-independent prostate cancer xenografts are stratified to similar treatment groups. Docetaxel serves as the positive control for both efficacy studies and is administered i.v. every 7 days for two doses of 10 mg/kg. Tumors are measured with calipers, and tumor volumes are calculated using the formula: TV= L×W2/2 where L is the largest diameter of the tumor and W is the smallest diameter perpendicular to L. Mice are followed for at least 1 week following the completion of the dosing so that tumor regrowth could be monitored.

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

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 4.0104 mL 20.0521 mL 40.1043 mL 100.2607 mL
    5 mM 0.8021 mL 4.0104 mL 8.0209 mL 20.0521 mL
    10 mM 0.4010 mL 2.0052 mL 4.0104 mL 10.0261 mL
    15 mM 0.2674 mL 1.3368 mL 2.6736 mL 6.6840 mL
    20 mM 0.2005 mL 1.0026 mL 2.0052 mL 5.0130 mL
    25 mM 0.1604 mL 0.8021 mL 1.6042 mL 4.0104 mL
    30 mM 0.1337 mL 0.6684 mL 1.3368 mL 3.3420 mL
    40 mM 0.1003 mL 0.5013 mL 1.0026 mL 2.5065 mL
    50 mM 0.0802 mL 0.4010 mL 0.8021 mL 2.0052 mL
    60 mM 0.0668 mL 0.3342 mL 0.6684 mL 1.6710 mL
    80 mM 0.0501 mL 0.2507 mL 0.5013 mL 1.2533 mL
    100 mM 0.0401 mL 0.2005 mL 0.4010 mL 1.0026 mL
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    10058-F4 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    10058-F4403811-55-2c-MycAutophagyMycInhibitorinhibitorinhibit

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