1. TGF-beta/Smad
  2. TGF-β Receptor

SB-431542 

Cat. No.: HY-10431 Purity: 99.24%
Data Sheet SDS Handling Instructions

SB-431542 is a potent and selective inhibitor of ALK5 and ALK4 with IC50 values of 94 nM and 14 nM, respectivelly, 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

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $88 In-stock
10 mg $80 In-stock
50 mg $300 In-stock
100 mg $560 In-stock
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Customer Review

    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: Mol Cell Biochem. 2017 Aug 12.

    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.

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    • Biological Activity

    • Protocol

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    • References

    Description

    SB-431542 is a potent and selective inhibitor of ALK5 and ALK4 with IC50 values of 94 nM and 14 nM, respectivelly, and is also an inhibitor of TGF-β Receptor.

    IC50 & Target

    IC50: 94 nM (ALK5), 140 nM (ALK4)

    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].

    References
    Preparing Stock Solutions
    Concentration Volume 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.
    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]

    SB-431542 is dissolved at a concentration of 10 mM in DMSO.

    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]

    SB-431542 is formulated in 20% DMSO/80% corn oil.

    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

    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

    Solvent & Solubility

    DMSO: ≥ 40 mg/mL; Ethanol: 11.17 mg/mL (Need ultrasonic and warming)

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.24%

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