1. TGF-beta/Smad
  2. TGF-β Receptor

SB-431542 

Cat. No.: HY-10431 Purity: 98.79%
Handling Instructions

SB-431542 is a potent and selective inhibitor of ALK5 with an IC50 value of 94 nM, and is also an inhibitor of TGF-β Receptor.

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

SB-431542 Chemical Structure

SB-431542 Chemical Structure

CAS No. : 301836-41-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
10 mg USD 96 In-stock
Estimated Time of Arrival: December 31
50 mg USD 360 In-stock
Estimated Time of Arrival: December 31
100 mg USD 672 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

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

    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 MCE. Usage Cited in: Mol Oncol. 2018 Mar;12(3):305-321.

    Western blot analysis of the expression level of EGFR, Sp1, total and phosphorylated Erk1/2 proteins in cell lysates from two breast cancer cells pretreated with PD98059 and then stimulated with TGF-β for the indicated times

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

    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 MCE. Usage Cited in: Mol Oncol. 2018 Mar;12(3):305-321.

    Western blot analysis of total and phosphorylated EGFR expression in two breast cancer cells pretreated with different concentration Erlotinib for 4h.

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

    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.

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

    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 MCE. Usage Cited in: Oncol Lett. 2017 Jul;14(1):541-546.

    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 MCE. Usage Cited in: Oncol Lett. 2018 Mar;15(3):2801-2806.

    A549 cells are co cultured with 10.0 mM Dexamethasone (DEX) with or without 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 MCE. Usage Cited in: Brain Res Bull. 2018 Feb 9;139:38-47.

    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 MCE. Usage Cited in: Int J Mol Sci. 2018 May 23;19(6).

    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 MCE. Usage Cited in: Oncol Lett. 2018 Jun;15(6):9681-9686.

    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 MCE. Usage Cited in: J Cell Mol Med. 2018 Sep;22(9):4354-4365.

    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 MCE. Usage Cited in: Stem Cells. 2018 Oct 29

    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 MCE. Usage Cited in: Stem Cells. 2018 Oct 29

    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 MCE. Usage Cited in: Phytother Res. 2018 Oct.

    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 MCE. Usage Cited in: Chin J Immun. 2016. 05. 002.

    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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    SB-431542 is a potent and selective inhibitor of ALK5 with an IC50 value of 94 nM, and is also an inhibitor of TGF-β Receptor.

    IC50 & Target

    IC50: 94 nM (ALK5)[2]

    In Vitro

    SB-431542 (1 μM) significantly reduces the TGF-β-induced nuclear accumulation of Smad proteins in A498 cells. SB-431542 inhibits TGF-β1-induced collagen Iα1 and PAI-1 mRNA with IC50 values of 60 and 50 nM, respectively. In addition, SB-431542 inhibits TGF-β1-induced fibronectin mRNA and protein with IC50 values of 62 and 22 nM, respectively[1]. SB-431542 (10 μM) is a selective inhibitor of endogenous activin and TGF-β signaling but has no effect on BMP signaling in NIH 3T3 cells[2]. TRKI, SB-431542, inhibits TGF-beta-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 attenuates the tumor-promoting effects of TGF-beta, including TGF-beta-induced EMT, cell motility, migration and invasion, and vascular endothelial growth factor secretion in human cancer cell lines. SB-431542 induces anchorage independent growth of cells that are growth-inhibited by TGF-beta, whereas it reduces colony formation by cells that are growth-promoted by TGF-beta[3]. SB-431542 (0.3 μM) inhibits cell proliferation induced by TGF-β in MG63 cells[4].

    In Vivo

    SB-431542 (10 mg/kg, i.p.) decreases lung metastasis but does not significantly alter growth of the primary tumor 4T1 xenograft[5].

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 40 mg/mL (104.06 mM)

    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
    10 mM 0.2602 mL 1.3008 mL 2.6015 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      SB-431542 is dissolved in 10% ethanol at a concentration of 0.5 mg/mL[6].

    References
    Kinase Assay
    [3]

    A total of 100,000 cells from each pool of A549 and HT29 are seeded into each well of 12-well plate. Cells are cultured in media containing 0.2% FBS for 18 hours, and then treated with 5 ng/mL TGF-β1 in the presence of SB-431542 (10 µM) in 0.5 mL of media for 24 hours. One hundred μLs of each supernatant media is used for VEGF assay according to the manufacturer's instruction. For TGF-β1 ELISA, 100,000 cells from each pool of A549, VMRC-LCD, and HT29 are seeded into each well of 12-well plates and serum-starved for 20 hours. Cells are then treated with SB-431542 in 0.5 mL of serum-free RPMI media for 24 hours. One hundred μLs of each supernatant media is activated and used for TGF-β1 assay according to the manufacturer's instruction.

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

    Cell Assay
    [1]

    A498 cells are seeded at 5,000 to 10,000 cells/well in 96-well plates. The cells are serum-deprived for 24 h and then treated with SB-431542 for 48 h to assess the cellular toxicity. Cell viability is determined by incubating cells for 4 h with XTT labeling and electron coupling reagent according to the manufacturer's directions. Live cells with active mitochondria produce an orange-colored product, formazan, which is detected using a plate reader at between A 450 nm and A 500 nm with a reference wavelength greater than 600 nm. The absorbance values correlate with the number of viable cells.

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

    Animal Administration
    [5]

    Ten thousand 4T1 cells are injected subcutaneously into the second mammary fat pad of 6-week-old Balb/c female mice. Tumors are measured twice weekly, and volume is calculated using the following formula: Volume = width2×length×0.52. Mice are randomly assigned to two treatment groups: control, n = 14 (20% DMSO/80% corn oil); SB-431542-treated, n = 15 (10 mg/kg body weight in 20% DMSO/80% corn oil, administered intraperitoneally three times per week starting one day after tumor cell inoculation. Primary tumors are resected when the volume at day 10 post-injection of 4T1 cells. All mice are monitored daily and euthanized after 4 weeks. The metastases are dissected to snap-freeze for further analysis.

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

    References
    Molecular Weight

    384.39

    Formula

    C₂₂H₁₆N₄O₃

    CAS No.

    301836-41-9

    SMILES

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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 98.79%

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    Product Name:
    SB-431542
    Cat. No.:
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    Cat. No.: HY-10431