2. TGF-beta/Smad
  3. TGF-β Receptor
  4. SB 525334

SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC50 of 14.3 nM.

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

SB 525334 Chemical Structure

SB 525334 Chemical Structure

CAS No. : 356559-20-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 72 In-stock
Solution
10 mM * 1 mL in DMSO USD 72 In-stock
Solid
1 mg USD 26 In-stock
5 mg USD 65 In-stock
10 mg USD 108 In-stock
50 mg USD 372 In-stock
100 mg USD 570 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 17 publication(s) in Google Scholar

SB 525334 Related Antibodies

Top Publications Citing Use of Products

    SB 525334 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2018 Dec 7;16(1):97.  [Abstract]

    Western blot analysis of LC3B, p62, HMGB1 and MHC protein expression in gastrocnemius muscles with the treatment of groups (TGF-β1, TGF-β1+SB525334, SB525334, TGF-β1+CQ, TGF-β1+si-HMGB1).

    SB 525334 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2018 Dec 7;16(1):97.  [Abstract]

    Immunofluorescence staining of LC3B and MHC in gastrocnemius in different groups (TGF-β1, TGF-β1+SB525334, SB525334, TGF-β1+CQ, TGF-β1+si-HMGB1) and HMGB1 staining of gastrocnemius.

    SB 525334 purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta. 2017 Dec 18;1864(3):721-734.  [Abstract]

    Microglial cells are incubated with or without TGF-β1 (5 ng/mL) and/or SB525334 (10 μM) for 24 h, followed by incubation with or without LPS for 24 h and subsequent NO determination.

    View All TGF-β Receptor Isoform Specific Products:

    View All Isoforms
    ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC50 of 14.3 nM.

    IC50 & Target

    IC50: 14.3 nM (ALK5)[1]
    In Vitro

    SB525334 (1 μM; for 15 minutes before stimulating with 0.625 ng/ml of TGF-β1, assesses after 6 days) inhibits TGF-β1-mediated proliferation of familial idiopathic pulmonary arterial hypertension (iPAH) pulmonary artery smooth muscle cells (PASMCs) at an IC50 of 295 nM [2].

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

    SB 525334 Related Antibodies

    Cell Proliferation Assay[2]

    Cell Line: PASMC cells
    Concentration: 1 μM
    Incubation Time: Pre-incubated for 15 minutes (before stimulating with 0.625 ng/ml of TGF-β1), assessed after 6 days
    Result: Inhibited TGF-β1-mediated proliferation of familial iPAH PASMCs at an IC50 of 295 nM.
    In Vivo

    SB525334 (3-30 mg/kg; p.o.; daily from days 17 to 35) significantly reverses pulmonary arterial pressure in a rat model of pulmonary arterial hypertension (PAH)[2].

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

    Animal Model: Adult male Sprague-Dawley rats (MCT rat model of pulmonary hypertension)[2]
    Dosage: 3, 30 mg/kg
    Administration: Oral administration; daily from days 17 to 35
    Result: Reduced the proportion of fully muscularized vessels to 28% at 3 mg/kg and returned fully muscularized vessel distribution beyond that seen at day 17 and approaching the phenotype observed in saline-exposed controls at 30 mg/kg.
    Molecular Weight

    343.42

    Formula

    C21H21N5
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    CC(C)(C1=NC(C2=CC=CC(C)=N2)=C(C3=CC=C4N=CC=NC4=C3)N1)C
    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 : 50 mg/mL (145.59 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 2.9119 mL 14.5594 mL 29.1189 mL
    5 mM 0.5824 mL 2.9119 mL 5.8238 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
    =
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    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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    Concentration (final)

    C2

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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: ≥ 2.5 mg/mL (7.28 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (7.28 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 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.

    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:  20% SBE-β-CD in Saline adjusted to pH 3.5 with HCL

      Solubility: 3 mg/mL (8.74 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

    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: 99.97%

    COA (255 KB) HNMR (258 KB) LCMS (266 KB) Elemental Analysis Report (114 KB)

    Handling Instructions (2659 KB)
    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 2.9119 mL 14.5594 mL 29.1189 mL 72.7972 mL
    5 mM 0.5824 mL 2.9119 mL 5.8238 mL 14.5594 mL
    10 mM 0.2912 mL 1.4559 mL 2.9119 mL 7.2797 mL
    15 mM 0.1941 mL 0.9706 mL 1.9413 mL 4.8531 mL
    20 mM 0.1456 mL 0.7280 mL 1.4559 mL 3.6399 mL
    25 mM 0.1165 mL 0.5824 mL 1.1648 mL 2.9119 mL
    30 mM 0.0971 mL 0.4853 mL 0.9706 mL 2.4266 mL
    40 mM 0.0728 mL 0.3640 mL 0.7280 mL 1.8199 mL
    50 mM 0.0582 mL 0.2912 mL 0.5824 mL 1.4559 mL
    60 mM 0.0485 mL 0.2427 mL 0.4853 mL 1.2133 mL
    80 mM 0.0364 mL 0.1820 mL 0.3640 mL 0.9100 mL
    100 mM 0.0291 mL 0.1456 mL 0.2912 mL 0.7280 mL
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    SB 525334 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:

    SB 525334356559-20-1SB525334SB-525334TGF-β ReceptorTransforming growth factor beta receptorsInhibitorinhibitorinhibit

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