2. TGF-beta/Smad
    Apoptosis
  3. TGF-β Receptor
    Apoptosis
  4. SB-431542

SB-431542 

Cat. No.: HY-10431 Purity: 99.89%
COA Handling Instructions

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

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 106 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 106 In-stock
Estimated Time of Arrival: December 31
Solid
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
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Customer Review

Based on 136 publication(s) in Google Scholar

Other Forms of SB-431542:

Top Publications Citing Use of Products

120 Publications Citing Use of MCE SB-431542

WB
RT-PCR

    SB-431542 purchased from MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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.

    View All TGF-β Receptor Isoform Specific Products:

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

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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].

    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].

    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

    Appearance

    Solid

    Formula

    C22H16N4O3
    CAS No.
    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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 250 mg/mL (650.38 mM; Need ultrasonic)

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

    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.

      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

    • 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

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.89%

    COA (252 KB) HNMR (216 KB) LCMS (121 KB)

    Handling Instructions (2659 KB)
    References
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    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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    Keywords:

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

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