2. TGF-beta/Smad
  3. TGF-β Receptor
  4. 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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10 mM * 1 mL in DMSO
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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 15 publication(s) in Google Scholar

Other Forms of RepSox:

RepSox Related Antibodies

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.

    View All TGF-β Receptor Isoform Specific Products:

    View All Isoforms
    ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 ACVR2A ACVR2B

    • 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.

    RepSox Related Antibodies

    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

    Appearance

    Solid

    Formula

    C17H13N5
    CAS No.
    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)

    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
    10 mM 0.3480 mL 1.7402 mL 3.4804 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 1.67 mg/mL (5.81 mM); Clear solution

    • 4.

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 1.67 mg/mL (5.81 mM); Clear solution

    • 5.

      Add each solvent one by one:  1% DMSO    99% Saline

      Solubility: ≥ 0.33 mg/mL (1.15 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.93%

    COA (252 KB) RP-HPLC (218 KB) Elemental Analysis Report (111 KB)

    Handling Instructions (2659 KB)
    References
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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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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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    × = ×
    C1   V1   C2   V2

    Keywords:

    RepSox446859-33-2E-616452 SJN 2511E616452E 616452SJN2511SJN 2511SJN-2511TGF-β ReceptorTransforming growth factor beta receptorsTGF-β signaling pathwaytransforming growth factor-beta receptor I (TGF-β-RI)activin like kinase 5 (ALK5)autophosphorylationobesitymetabolictype 2 diabetesInhibitorinhibitorinhibit

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