1. TGF-beta/Smad
  2. TGF-β Receptor
  3. SB-505124

SB-505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.

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SB-505124 Chemical Structure

SB-505124 Chemical Structure

CAS No. : 694433-59-5

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10 mM * 1 mL in DMSO
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10 mg USD 158 In-stock
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Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of SB-505124:

Top Publications Citing Use of Products

    SB-505124 purchased from MedChemExpress. Usage Cited in: Oncogene. 2019 Mar;38(12):2056-2075.  [Abstract]

    Treatment with SB505124 for 3 days significantly increases apoptosis at 4 and 8 μM in WERI Rb1.

    SB-505124 purchased from MedChemExpress. Usage Cited in: Oncogene. 2019 Mar;38(12):2056-2075.  [Abstract]

    Treatment with SB505124 for 3 days significantly increases apoptosis at 4 and 8 μM in WERI Rb1.

    SB-505124 purchased from MedChemExpress. Usage Cited in: Oncogene. 2019 Mar;38(12):2056-2075.  [Abstract]

    The effects on growth and invasion are paralleled by a dose-dependent inhibition in SMAD2 phosphorylation upon treatment with SB505124 at 0.5, 1, 2, 3, 4, 8 μM for 4 days.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    SB-505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.

    IC50 & Target

    IC50: 129 nM (ALK4), 47 nM (ALK5)

    In Vitro

    SB-505124 demonstrates no toxicity to renal epithelial A498 cells at concentrations up to 100 μM for 48 h. 505124 inhibits the closely related ALK4 with an IC50 value of 129±11 nM (about 2.5-fold less sensitive than ALK5) but does not inhibit ALK2 at concentrations up to 10 μM. SB-505124 (1 μM) inhibits the TGF-β-induced phosphorylation of Smad2 in all three of these cell lines in a concentration-dependent fashion. SB-505124 (1 or 5 μM) potently inhibits TGF-β-induced activation of JNK/SAP, extracellular signal-regulated kinase 1/2, and p38 despite the different patterns of activation in these cells[1]. SB-505124 (10 μM) impairs Smad2 phosphorylation and CTGF and α-SMA expression in vitro[2]. SB-505124 susspresses CTGF and α-SMA observed by immunofluorescence. Cell outgrowth from explants dissected from eyes to which SB-505124 is applied during GFS is robust while outgrowth is poor from those treated with MMC[3].

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

    In Vivo

    SB-505124 (5 mg/kg; i.p.) alone has no effect in C57Bl6 mice with A549 xenografts, but administration of SB-505124 with a single dose of Carboplatin (60 mg/kg) results in durable responses without the need for maintenance therapy in five animals[4].

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

    Animal Model: C57Bl6 mice with A549 xenografts[4]
    Dosage: 5 mg/kg
    Administration: I.p.; daily
    Result: Had no effect alone, but administration with a single dose of carboplatin (60 mg/kg) resulted in durable responses without the need for maintenance therapy in five animals.
    Molecular Weight

    335.40

    Formula

    C20H21N3O2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC1=CC=CC(C2=C(C3=CC=C(OCO4)C4=C3)N=C(C(C)(C)C)N2)=N1

    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 : 113.33 mg/mL (337.90 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 2.9815 mL 14.9076 mL 29.8151 mL
    5 mM 0.5963 mL 2.9815 mL 5.9630 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: ≥ 2.5 mg/mL (7.45 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (7.45 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (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:
    %
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    %
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    %
    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
    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 2.9815 mL 14.9076 mL 29.8151 mL 74.5379 mL
    5 mM 0.5963 mL 2.9815 mL 5.9630 mL 14.9076 mL
    10 mM 0.2982 mL 1.4908 mL 2.9815 mL 7.4538 mL
    15 mM 0.1988 mL 0.9938 mL 1.9877 mL 4.9692 mL
    20 mM 0.1491 mL 0.7454 mL 1.4908 mL 3.7269 mL
    25 mM 0.1193 mL 0.5963 mL 1.1926 mL 2.9815 mL
    30 mM 0.0994 mL 0.4969 mL 0.9938 mL 2.4846 mL
    40 mM 0.0745 mL 0.3727 mL 0.7454 mL 1.8634 mL
    50 mM 0.0596 mL 0.2982 mL 0.5963 mL 1.4908 mL
    60 mM 0.0497 mL 0.2485 mL 0.4969 mL 1.2423 mL
    80 mM 0.0373 mL 0.1863 mL 0.3727 mL 0.9317 mL
    100 mM 0.0298 mL 0.1491 mL 0.2982 mL 0.7454 mL
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    SB-505124 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:
    SB-505124
    Cat. No.:
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