SB-431542 [301836-41-9]

Cat# HY-10431-10mg

Size : 10mg

Brand : MedChemExpress

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SB-431542 est un inhibiteur puissant et sélectif du récepteur ALK5 / TGF-β de type I avec une valeur IC50 de 94 nM.

SB-431542 ist ein wirksamer und selektiver Inhibitor des ALK5/TGF-β-Typ I-Rezeptors mit einem IC50 -Wert von 94 nM.

SB-431542 is a TGF-β receptor kinase inhibitor (TRKI). SB-431542 has inhibitory activity for ALK4, ALK5 and ALK7 with IC50 values of 1 μM, 0.75 μM and 2 μM, respectively. SB-431542 also inhibits TGF-β-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 can be used for the research of cancer and signal transduction pathways.

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

SB-431542 Chemical Structure

SB-431542 Chemical Structure

CAS No. : 301836-41-9

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

Based on 179 publication(s) in Google Scholar

Other Forms of SB-431542:

  • SB-431542 (GMP) In-stock

    SB-431542 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2023 Mar 16;161:114537.  [Abstract]

    SB431542 (4.2 mg/kg; i.p.; single daily for 3 days) reduces the expression of α-SMA, collagen-I and p-Smad3 in SiO2-induced fibrosis lungs of mice.

    SB-431542 purchased from MedChemExpress. Usage Cited in: Stem Cells. 2019 Feb;37(2):190-201.  [Abstract]

    Western blot analyses show the repression of SMC specific markers in the sh-GPM6B TGF-β1 group are abolished by Alantolactone in the sh-GPM6B and the enrichment of SMC specific markers in the GPM6B-sgRNA cells is cancelled by treatment with SB431542.

    SB-431542 purchased from MedChemExpress. Usage Cited in: Stem Cells. 2019 Feb;37(2):190-201.  [Abstract]

    Western blot images show Smad2/3 phosphorylation is lower than baseline in the sh-GPM6B cells and higher than baseline in the GPM6B-sgRNA cells. The phosphorylation of Smad2/3 in the sh-GPM6B TGF-β1 group is elevated by Alantolactone and the phosphorylation is reduced by treatment with SB431542.

    SB-431542 purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2019 Mar;19(3):2107-2114.  [Abstract]

    Effects of the TGF‑β1 inhibitor SB (20 μM) on mechanical force‑induced COL‑1 and MMP‑1 mRNA expression.

    SB-431542 purchased from MedChemExpress. Usage Cited in: Phytother Res. 2019 Jan;33(1):214-223.  [Abstract]

    Western analysis of FN and α-SMA in cardiac fibroblasts or NIH3T3 with treatments of (+)‐isobicyclogermacrenal, spathulenol, oxymatrine (OMT), and SB431542 at indicated concentrations.

    SB-431542 purchased from MedChemExpress. Usage Cited in: Mol Oncol. 2018 Mar;12(3):305-321.  [Abstract]

    Western blot analysis of EGFR, total and phosphorylated Smad3, total and phosphorylated ERK protein expression in cell lysates from two breast cancer cells pretreated with SB431542 and then stimulated with TGF-β for the indicated times.

    SB-431542 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2018 May 23;19(6). pii: E1556.  [Abstract]

    E-cadherin, N-cadherin, Snail, and MMP-2 expression in HCC cells is examined by Western blot analysis. GAPDH is used as a loading control.

    SB-431542 purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2018 Sep;22(9):4354-4365.  [Abstract]

    p-FOXO3a (Thr32), p-FOXO3a (Ser253), FOXO3a, p-Akt and Akt expression via western blot following treatment with PBS, ASV, TGF-b1, TGF-b1+ASV, TGF-b1+SB431542 or TGF-b1+LY294002.

    SB-431542 purchased from MedChemExpress. Usage Cited in: Immunol Lett. 2019 Feb;206:33-40.  [Abstract]

    Monocytes were cultured with 20 ng/mL M-CSF with or without 10 ng/mL TGF-β1 for 2 days, with SB431542 (1 or 50 μM) or SIS3 (2.5 μM) having been added 30 min beforehand. Whole-cell lysates were subjected to SDS-PAGE and immunoblotted.

    SB-431542 purchased from MedChemExpress. Usage Cited in: Mol Cell Biochem. 2018 Feb;439(1-2):117-129.  [Abstract]

    Protein expression levels of E-cadherin N-cadherin, p-ERK, ERK, TGF-β1, p-Smad2, and p-Smad3 in each group are analyzed by western blotting.

    SB-431542 purchased from MedChemExpress. Usage Cited in: Brain Res Bull. 2018 May;139:38-47.  [Abstract]

    pSmad2/3 protein levels are down-regulated by the ALK5 inhibitor SB431542 (rGDF11 group vs. rGDF11+SB group, p=0.000).

    SB-431542 purchased from MedChemExpress. Usage Cited in: Oncol Lett. 2018 Mar;15(3):2801-2806.  [Abstract]

    A549 cells are co cultured with 10.0 mM SB431542 for 48 h, the expression of TGF β1, Smad2 and caspase 3 are tested by western blot analysis and then analyzed.

    SB-431542 purchased from MedChemExpress. Usage Cited in: Oncol Lett. 2018 Jun;15(6):9681-9686.  [Abstract]

    A549 cells are treated with 1.0% CSE with or without 10.0 mM SB431542 for 48 h, the levels of TGF β1, p Smad2, and MMP3 is assayed by western blot analysis.

    SB-431542 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2017 Apr 18;18(4). pii: E853.  [Abstract]

    The protein level of Six2 and Ki67 after the treatment of phosphorylation Smad3 ( p-Smad3) inhibitor SB431542 (10 µM) for 48 h.

    SB-431542 purchased from MedChemExpress. Usage Cited in: Oncol Lett. 2017 Jul;14(1):541-546.  [Abstract]

    To investigate the effect of SB431542 on the accumulation of TGFβ1 and MMP3 in MM cells, RPMI 8226 cells are treated with 10, 100 and 1,000 nmol/mL SB431542 for 48 h. Western blotting is performed. The results demonstrate that SB431542 significantly decreases the accumulation of TGFβ1 and MMP3 at 100 and 1,000 nmol/mL when compared with the control. Smad2, as a signaling molecule, can be initially activated by TGFβ1. Therefore, the effect of SB431542 on the expression of Smad2 and p-Smad2 in RPM

    SB-431542 purchased from MedChemExpress. Usage Cited in: Chin J Immun. 2016 (5): 615-619.

    10-1000 nM of SB431542 are co-cultured with RLE-6TN cells for 48 h. Expressions of p-Smad2 and Smad are detected by Western blot.

    SB-431542 purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2015 Sep;28(1):707-14.  [Abstract]

    SB431542 is used to block the TGF-β1/Smad2 pathway and the expression of PLTP, p-Smad2 and cleaved caspase-3 is analyzed. (A) RLE-6TN cells are treated with 5–500 nM SB431542 for 72 h. Expression of PLTP and p-Smad2 is analyzed by Western blot. (B) CSE-treated rat lung epithelial cells are treated with 500 nM SB431542 to block the TGF-β1/Smad2 pathway.

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    Description

    SB-431542 is a TGF-β receptor kinase inhibitor (TRKI). SB-431542 has inhibitory activity for ALK4, ALK5 and ALK7 with IC50 values of 1 μM, 0.75 μM and 2 μM, respectively. SB-431542 also inhibits TGF-β-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 can be used for the research of cancer and signal transduction pathways[1][2][3].

    IC50 & Target[1]

    ALK4

    1 μM (IC50)

    ALK5

    0.75 μM (IC50)

    ALK7

    2 μM (IC50)

    In Vitro

    SB-431542 can inhibit the activity for ALK4, ALK5 and ALK7 with IC50 values of 1 μM, 0.75 μM and 2 μM, respectively[1].
    SB-431542 (0- 10 μM; 24 h) inhibits ALK5 and also the activin type I receptor ALK4 and the nodal type I receptor ALK7, which are very highly related to ALK5 in their kinase domains[1].
    SB-431542 (0.1, 0.5, 1, 5, or 10 μM; 30 min) efficiently inhibits Smad phosphorylation induced by TGF-β and activin but not BMP4[1].
    SB-431542 (0-10 μM) inhibits TGF-beta-induced transcription, gene expression, apoptosis, and growth suppression[2].

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

    Western Blot Analysis[1]

    Cell Line: NIH 3T3 cells; HaCaT, NIH 3T3, C2C12 cells and T47D cells
    Concentration: 10 μM; 0.1, 0.5, 1, 5, or 10 μM
    Incubation Time: 24 h; 30 min
    Result: Inhibited efficiently phosphorylated Smad2.
    Inhibited the TGF-β- and activin-induced phosphorylation of Smad2 but not BMP-induced phosphorylation of Smad1.

    Apoptosis Analysis[2]

    Cell Line: A549 and HT29 cells
    Concentration: 10 μM
    Incubation Time: 24 h
    Result: Inhibited TGF-induced growth suppression and apoptosis.

    Cell Invasion Assay[2]

    Cell Line: A549 cells
    Concentration: 2, 10 μM
    Incubation Time: 21 h
    Result: Blocked TGF- induced tumor cell invasion.

    Cell Migration Assay [2]

    Cell Line: A549 cells
    Concentration: 2, 10 μM
    Incubation Time: 5 h , 30 h
    Result: Blocked TGF- induced tumor cell migration.
    In Vivo

    SB-431542 (subconjunctival; 0.5 and 2 mM; on days 1, 2, 3, and 7) inhibits scar formation after glaucoma filtration surgery in New Zealand rabbits[3].

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

    Animal Model: Rabbits (3 to 5 months, 1.8 - 2.5 kg)[3]
    Dosage: 0.5 and 2 mM
    Administration: Subconjunctival injection, on days 1, 2, 3, and 7
    Result: Showed wound healing and less severe scar formation.
    Molecular Weight

    384.39

    Formula

    C22H16N4O3

    CAS No.

    301836-41-9

    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    O=C(C1=CC=C(C=C1)C2=NC(C3=CC=C4OCOC4=C3)=C(N2)C5=NC=CC=C5)N

    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 : ≥ 100 mg/mL (260.15 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 11.17 mg/mL (29.06 mM; Need ultrasonic and warming)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6015 mL 13.0076 mL 26.0152 mL
    5 mM 0.5203 mL 2.6015 mL 5.2030 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: ≥ 2.08 mg/mL (5.41 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.41 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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

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    (per animal)

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    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: 99.89%

    References
    • [1]. Gareth J Inman, et al. SB-431542 is a potent and specific inhibitor of transforming growth factor-beta superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7. Mol Pharmacol. 2002 Jul;62(1):65-74.  [Content Brief]

      [2]. Sunil K Halder, et al. A specific inhibitor of TGF-beta receptor kinase, SB-431542, as a potent antitumor agent for human cancers. Neoplasia. 2005 May;7(5):509-21.  [Content Brief]

      [3]. Yi-qin Xiao, et al. SB-431542 inhibition of scar formation after filtration surgery and its potential mechanism. Invest Ophthalmol Vis Sci. 2009 Apr;50(4):1698-706.  [Content Brief]

    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
    Ethanol / DMSO 1 mM 2.6015 mL 13.0076 mL 26.0152 mL 65.0381 mL
    5 mM 0.5203 mL 2.6015 mL 5.2030 mL 13.0076 mL
    10 mM 0.2602 mL 1.3008 mL 2.6015 mL 6.5038 mL
    15 mM 0.1734 mL 0.8672 mL 1.7343 mL 4.3359 mL
    20 mM 0.1301 mL 0.6504 mL 1.3008 mL 3.2519 mL
    25 mM 0.1041 mL 0.5203 mL 1.0406 mL 2.6015 mL
    DMSO 30 mM 0.0867 mL 0.4336 mL 0.8672 mL 2.1679 mL
    40 mM 0.0650 mL 0.3252 mL 0.6504 mL 1.6260 mL
    50 mM 0.0520 mL 0.2602 mL 0.5203 mL 1.3008 mL
    60 mM 0.0434 mL 0.2168 mL 0.4336 mL 1.0840 mL
    80 mM 0.0325 mL 0.1626 mL 0.3252 mL 0.8130 mL
    100 mM 0.0260 mL 0.1301 mL 0.2602 mL 0.6504 mL
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    SB-431542 Related Classifications

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    Keywords:

    SB-431542301836-41-9SB431542SB 431542OrganoidTGF-β ReceptorApoptosisTransforming growth factor beta receptorsTGF-β receptor kinase inhibitor (TRKI)ALK4ALK5ALK7transcriptiongene expressionapoptosisgrowth suppressioncancersignal transduction pathwaysInhibitorinhibitorinhibit

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