1. Stem Cell/Wnt TGF-beta/Smad
  2. Organoid TGF-β Receptor
  3. RepSox

RepSox  (Synonyms: E-616452; SJN 2511)

Cat. No.: HY-13012 Purity: 99.93%
COA Handling Instructions

RepSox (E-616452) is a potent and selective transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes.

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

RepSox Chemical Structure

RepSox Chemical Structure

CAS No. : 446859-33-2

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 85 In-stock
Solid
5 mg USD 77 In-stock
10 mg USD 99 In-stock
50 mg USD 385 In-stock
100 mg USD 660 In-stock
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Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of RepSox:

Top Publications Citing Use of Products

    RepSox purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Jun 19;8(36):60159-60172.  [Abstract]

    SH-SY5Y (A) and HEK293 cells (B) are treated with 25 μM RepSox (Rep) in absence or presence of dPA or dPPA for 72 h, and the Western blotting results show that dPA or dPPA increases the expression in the presence of RepSox. RepSox does not cause significant alteration of furin protein compared to control. The expression of furin remains significantly increased after dPA or dPPA in the presence of RepSox.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    RepSox (E-616452) is a potent and selective transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes[1][2].

    IC50 & Target

    ALK5

    4 nM (IC50)

    In Vitro

    RepSox (compound 19) inhibits ALK5 autophosphorylation with an IC50 value of 4 nM[1].
    RepSox (0-10 μM; 0-8 days) induces adipogenesis from mouse embryonic fibroblasts (MEFs) in fibroblast culture medium[2].
    RepSox (0-10 μM; 0-8 days) promotes the differentiation of the brown fat precursor cells and induce browning of the white fat precursor cells[2].
    RepSox(0-10 μM; 0-8 days) induces brown adipogenesis in primary mouse fibroblasts and fat precursor cells[2].

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

    Western Blot Analysis[2]

    Cell Line: Mouse embryonic fibroblasts (MEFs)
    Concentration: 3 μM
    Incubation Time: 0-8 days
    Result: Showed upregulation of UCP1 protein levels.

    Immunofluorescence[2]

    Cell Line: MEFs
    Concentration: 3 μM
    Incubation Time: 0-8 days
    Result: Increased the number of mitochondria in MEF-derived adipocytes and significantly increased UCP1 levels.

    RT-PCR[2]

    Cell Line: MEFs
    Concentration: 3 μM
    Incubation Time: 0-8 days
    Result: Induced the activation of a network of genes controlling adipogenesis, energy expenditure, and the thermogenic program in MEFs.
    Molecular Weight

    287.32

    Formula

    C17H13N5

    CAS No.
    Appearance

    Solid

    Color

    Light brown to yellow

    SMILES

    CC1=NC(C2=NNC=C2C3=NC4=CC=CN=C4C=C3)=CC=C1

    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 : 33.33 mg/mL (116.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.4804 mL 17.4022 mL 34.8044 mL
    5 mM 0.6961 mL 3.4804 mL 6.9609 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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: ≥ 7.5 mg/mL (26.10 mM); Clear solution

      This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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: ≥ 7.5 mg/mL (26.10 mM); Clear solution

      This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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)

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    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: 99.93%

    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 3.4804 mL 17.4022 mL 34.8044 mL 87.0110 mL
    5 mM 0.6961 mL 3.4804 mL 6.9609 mL 17.4022 mL
    10 mM 0.3480 mL 1.7402 mL 3.4804 mL 8.7011 mL
    15 mM 0.2320 mL 1.1601 mL 2.3203 mL 5.8007 mL
    20 mM 0.1740 mL 0.8701 mL 1.7402 mL 4.3505 mL
    25 mM 0.1392 mL 0.6961 mL 1.3922 mL 3.4804 mL
    30 mM 0.1160 mL 0.5801 mL 1.1601 mL 2.9004 mL
    40 mM 0.0870 mL 0.4351 mL 0.8701 mL 2.1753 mL
    50 mM 0.0696 mL 0.3480 mL 0.6961 mL 1.7402 mL
    60 mM 0.0580 mL 0.2900 mL 0.5801 mL 1.4502 mL
    80 mM 0.0435 mL 0.2175 mL 0.4351 mL 1.0876 mL
    100 mM 0.0348 mL 0.1740 mL 0.3480 mL 0.8701 mL
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    RepSox 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.

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    Product Name:
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    Cat. No.:
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