SB431542

Catalog No.S1067

SB431542 Chemical Structure

Molecular Weight(MW): 384.39

SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM in a cell-free assay, 100-fold more selective for ALK5 than p38 MAPK and other kinases.

Size Price Stock Quantity  
In DMSO USD 143 In stock
USD 110 In stock
USD 470 In stock
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9 Customer Reviews

  •  

    Hedgehog, Igf and Tgf signaling are required for myocardial regeneration in zebrafish. (C) Quantification of the effects of CyA (10 uM), NVP AEW541 (2 uM) and SB-431542 (10 uM) on cardiomyocyte proliferation after resection injury. Fish were treated from 6 to 7 dpa. (D) Quantification of the effects of CyA, NVP AEW541 and SB-431542 on proliferation after genetic cardiomyocyte ablation.

    Development 2013 140, 660-666. SB431542 purchased from Selleck.

    Long-term response of SB431542 and SB203580 release from scaffold implants. Histological results of H&E staining showing the capsule thickness of the various treatments at 14 days. The scale bar shows 100 uM and is applicable to all images in the panel. In each bar graph the tissue and cellular response to SB431542 were found to be significant from the control. For each treatment group six animals were tested. Statistics are performed by ANOVA with Bonferroni comparisons and taken to be significant at ∗∗P < 0.01.

    Acta Biomater 2014 10(7):3108-16. SB431542 purchased from Selleck.

  • Transforming growth factor-b (TGF-b)/Smad3 induces Akt phosphorylation in vascular smooth muscle cells (SMCs). C: vascular SMCs were pretreated with the TGF- receptor inhibitor SB431542 (10 uM) for 30 min and then stimulated with TGF- (5 ng/ml) for 12 h, and p-Akt was measured by Western blot analysis.

    Am J Physiol Heart Circ Physiol 2012 302, H2211-H2219. SB431542 purchased from Selleck.

     

    Effect of small molecule inhibitors on reprogramming efficiency of myoblast cell derived from 5 different donors. (A) Reprogramming efficiency is shown as number of colonies from 10^5 starting cells on Y-axes. Ctrl, control condition and addition of small molecule inhibitors are marked. (B) AP staining of reprogrammed myoblast cell lines, from 5 different donors, in wells of 12-well plates at day 18. Ctrl, control condition and additions of small molecule inhibitors are marked.

    Stem Cells Dev 2013 SB431542 purchased from Selleck.

  • Retroviral reprogramming of myoblasts. (C) Small molecule inhibitors effect on reprogramming efficiency compared to control. (D) AP staining of reprogrammed plates with or without inhibitors. Close-up of AP staining, bar 500 um; AP, alkaline phosphatase.

    Stem Cells Dev 2013 SB431542 purchased from Selleck.

     

    TGFb1 mRNA expression in different follicles of the 26 weeks old hen ovaries and its effect on CTGF mRNA expression in granulosa cells. Effects of TGFb1 and inhibitor SB431542 on CTGF mRNA expression in granulosa cells from F2 to F4 and POF1 follicles.

    Gen Comp Endocr 2012 178, 314–322. SB431542 purchased from Selleck.

  • SB431542 inhibit expression of TGF-beta induced pS2 in MvILu cell

     

     

    Dr. Kah-Wai Lin of Karolinska Biomics Center. SB431542 purchased from Selleck.

    SB431542 purchased from Selleck.

  • (C) C3H10T1/2 cells transfected with pEF-BOS or pEF-Flag-TAZ were cultured for 8 days in osteogenic medium (OM) including ascorbic acid and β-glycerophosphate in the absence or presence of TGF-β inhibitors (SB-431542 or SB-525334). ALP activity was measured in the cell layer and normalized to cellular protein content. Data are expressed as means 6 ± SD ( *p < 0.05 vs. pEF-BOS, # p < 0.01 vs. vehicle) (D) Quantitative RT-PCR analysis of Col 1 and ALP in C3H10T1/2 cells.

    SB431542 purchased from Selleck.

Purity & Quality Control

Choose Selective TGF-beta/Smad Inhibitors

Biological Activity

Description SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM in a cell-free assay, 100-fold more selective for ALK5 than p38 MAPK and other kinases.
Targets
ALK4 [2]
(Cell-free assay)
ALK7 [2]
(Cell-free assay)
ALK5 [1]
(Cell-free assay)
94 nM
In vitro

SB 431542 inhibits the activin type I receptor ALK4 and the nodal type I receptor ALK7, which are responsible for the phosphorylation of Smad2. SB 431542 has little effect on ALK1, ALK2, ALK3, and ALK6, which show phosphorylation of Smad1. SB 431542 is a selective inhibitor of endogenous activin but has no apparent effect on BMP signaling. SB 431542 could induce both Smad2/Smad4- and Smad3/Smad4-dependent transcription. [2] In A498 cells, SB 431542 inhibits both TGF-β1-induced collagen Iα1 and PAI-1 mRNA with IC50 of 60 nM and 50 nM, respectively. In addition, SB 431542 inhibits production of TGF-β1-induced fibronectin mRNA and protein with IC50 of 62 nM and 22 nM, respectively. [3] SB 431542 blocks the TGF-β-mediated growth factors, including PDGF-A, FGF-2 and HB-EGF, leading to an increase in proliferation of MG63 cells. SB 431542 also inhibits TGF-β-induced c-Myc and p21 WAF1/CIP1. [4] SB 431542 significantly suppresses TGF-β-induced G1 arrest, leading to accumulation of cells in the S phase of the cell cycle in FET, RIE, and Mv1Lu cells. SB 431542 also inhibits TGF-β-induced epithelial to mesenchymal transition (EMT) in NMuMG and PANC-1 cells. [5] SB 431542 significantly elevates the expression of CD86 in BM-DCs and that of CD83 within CD11c+ cells suppressed by TGF-β. SB 431542 is able to induce NK activity through functional maturation and IL-12 production of human DCs. [6]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293T MV3GeY5kfGmxbjDBd5NigQ>? MW[xNEDPxE1? M4HlXVIzKGh? M2Dm[mROW09? NV\HO3o1UW6qaXLpeJMhXEeEUkKgd4lodmGuaX7nJIlvKGi3bXHuJGhGUzJ7M2SgZ4VtdHNiYYPz[ZN{\WRiYYOgTY5pcWKrdHnvckBw\iCVTVHEJIFkfGm4YYTpc44hf2m2aDDJR|UxKG:oIECuNFY3|ryP M4ryUFI{OTNyNkK2
H1299 MXHNbYdz[XSrb36gRZN{[Xl? MVexJO69VQ>? MXixNk0zPCCq MYPEUXNQ NYPnb5VUUW6mdXPld{BidnSrbXnndoF1d3K7IHHjeIl3cXS7IHHnZYlve3RiaIXtZY4hUDF{OUmgZ4VtdHNiYYPz[ZN{\WRiYYOgTY5pcWKrdHnvckBw\iClZXzsJI1q\3KjdHnvckB4cXSqIFnDOVAhd2ZiMD61{txO MXKyOFQyPzR5OR?=
HaCaT MUnGeY5kfGmxbjDBd5NigQ>? M4HxTlMvOi13MDFOwG0> MYOxOUBucW5? MUPEUXNQ NEPhRmdKdmirYnn0d{BVT0[kZYThJJJm[2WydH;yJIlvKGi3bXHuJGhiS2GWIHPlcIx{KGG|c3Xzd4VlKGG|IGPtZYQheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkG3Nu69VQ>? M4DJUlIxQTF7Nke4
HepG2 NHfnVJVHfW6ldHnvckBCe3OjeR?= NGrTeXUyOiCq Mm\5SG1UVw>? Ml7nTY5pcWKrdIOgWGdHWi1zIHnuJIh2dWGwIFjldGczKGOnbHzzJIV5eHKnc4PpcochWEGLLXz1Z4ln\XKjc3Wge4l1cCCLQ{WwJI9nKDBwMkZOwG0> NF3iNmQyQTlzNEC2PC=>
CHO-HIR NH\yellHfW6ldHnvckBCe3OjeR?= MXqwMlAyNTNizszN NYX0XlR7OiCq NYG3fFM6TE2VTx?= MYPJcohq[mm2czDUS2Zj\XSjLXnu[JVk\WRiZH;3cpN1emWjbTD0doFve2O{aYD0bY9v[WxiYXP0bZZifGmxbjDv[kBCVEt3IHX4dJJme3OnZDDpckBEUE9vSFnSJINmdGy|IHHzd4V{e2WmIHHzJIlvfHKjY3XscJVt[XJidILhcpNtd2OjdHnvckBw\iCHR1\QMXNu[WR{IIfpeIghUUN3MDDv[kAxNjN3zszN NW[3d5dFOjRyNUWwOFY>
Sf9 MkLGSpVv[3Srb36gRZN{[Xl? M2e4dlIhcA>? MYTEUXNQ MV7Jcohq[mm2czDoeY1idiC{ZXPvcYJqdmGwdDDBUGs2KHCqb4PwbI9zgWyjdHnvckBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IIfpeIghUUN3MDDv[kAyNjV2Mt88US=> NVXr[pVUOTd3NUK1NFc>
C32 NIDuN5dHfW6ldHnvckBCe3OjeR?= M2X2T|ExKM7:TR?= NIPPXoQzOGh? M3\lSGlvcGmkaYTzJHRzgXCjbn;zc41iKGO{dYrpJHkhcW6oZXP0bY9vNWmwZIXj[YQhXEeIYnX0ZUB{cWewYXzpcochcW5ibXnub{BEOzJiY3XscJMh[XRiMUCgeW0> M3r2NVE4PTJ4N{W3
Mouse embryo cardiomyocytes MWPGeY5kfGmxbjDBd5NigQ>? NXL2SZIyOTBizszN MV6xJIg> NYDxWXVKUW6qaXLpeJMhcW64YYPpc44hd2ZiVIL5dIFvd3OxbXGgZ5J2gmliWTDpckBud3W|ZTDlcYJzgW9iY3Hy[IlwdXmxY4n0[ZMh[XO|ZYPz[YQh[XNicHH0bI9o\W5iaX7m[YN1cW:wIHH0JFExKHWP NG\wUFAyPzV{Nke1Oy=>
Mouse embryo cardiomyocytes MXzGeY5kfGmxbjDBd5NigQ>? NXvZUnEyOTBizszN M{PPWVEhcA>? NHvUT5FKdmirYnn0d{BVT0ZvYnX0ZU0yNWmwZIXj[YQhW22jZEKgdIhwe3Cqb4L5cIF1cW:wIHnuJI1wfXOnIHXtZpJ6dyClYYLkbY9ugW:leYTld{BifCBzMDD1US=> NIfS[XMyPzV{Nke1Oy=>
Mouse embryo cardiomyocytes MWTGeY5kfGmxbjDBd5NigQ>? NFzWWnkyOCEQvF2= MW[xJIg> NV7R[4NVUW6qaXLpeJMhXHK7cHHuc5NwdWFiY4L1fokhTG1{OFOgbY5n\WO2aX;uMYlv\HWlZXSgV41i\DJicHjvd5Bpd3K7bHH0bY9vKGmwIH3veZNmKGWvYoL5c{Bk[XKmaX;tfY9kgXSnczDheEAyOCC3TR?= NI\ZT4IyPzV{Nke1Oy=>
Trypanosoma cruzi trypomastigotes NH7JWYRCdnSrbXnjdo9jcWGuIFHzd4F6 NY\QeGRKOTBizszN M1HCOVQhcA>? NX;FO443UW6mdXPld{BidnSrdIL5dIFvd3OxbXHsJIFkfGm4aYT5JIFo[Wmwc4SgWJJ6eGGwb4PvcYEh[3K3enmgeJJ6eG:vYYP0bYdwfGW|IHHzd4V{e2WmIHHzJIVn\mWldDDvckBx[XKjc3n0[UBud3KyaH;sc4d6KGG2IEGwJJVO M1vaflE4PTJ4N{W3
Mouse cardiomyocytes Mny2RY51cW2rY4LvZolidCCDc4PhfS=> M3W4V|ExKM7:TR?= NXPxb5h5PCCq MYDJcoR2[2W|IHHueIl1enmyYX7vd49u[WxiYXP0bZZqfHliYXfhbY5{fCCWconwZY5we2:vYTDjdpV7cSC\IHnuJI1wfXOnIHPhdoRqd227b3P5eIV{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBqdnS{YXPlcIx2dGG{IHHtZZN1cWexdHXzJIF1KDFyIIXN M{XKZ|E4PTJ4N{W3
Mouse cardiomyocytes NWDaVFdHSW62aX3pZ5Jw[mmjbDDBd5NigQ>? MVSxNEDPxE1? NIe5fXQ6PiCq NYO4PFBYUW6mdXPld{BidnSrdIL5dIFvd3OxbXHsJIFkfGm4aYT5JIFo[Wmwc4SgWJJ6eGGwb4PvcYEh[3K3enmgXUBqdiCvb4Xz[UBk[XKmaX;tfY9kgXSnczDhd5Nme3OnZDDhd{BKdmirYnn0bY9vKG:oIITyfZBwdWG|dHnnc5RmKHKnbHXhd4Uh[XRiMUCgeW0> MoC1NVc2OjZ5NUe=
HaCaT M2XsZ2Z2dmO2aX;uJGF{e2G7 M3P3OFAvODVizszN NHzPZlAzKGh? NXjRSGFQTE2VTx?= MlfOSI9meyCwb4SgbY5pcWKrdDDUS2Yu[mW2YTDpcoR2[2WmIFHMT|Uh[WO2aY\peJkhcW5iSHHDZXQh[2WubIOgZZN{\XO|ZXSgZZMheDOWUD3seYNq\mW{YYPlJJJmeG:{dHXyJIFkfGm4aYT5JIF1KDBwMEWgeW0> MWixO|U2OjVyNx?=

... Click to View More Cell Line Experimental Data

In vivo SB 431542 triggers cytotoxic T lymphocyte (CTL) activities in the colon-26 carcinoma models and is most likely to produce antitumor immunological outcomes through alteration of DC function suppressed by TGF-β. [6]

Protocol

Kinase Assay: [1]
+ Expand

Flashplate assay for ALK5:

SB 431542 is dissolved in DMSO at a concentration of 10 mM. The kinase domain of TGFβRI, from amino acid 200 to the C-terminus, and the full-length Smad3 protein are expressed as N-terminal glutathion S-transferase (GST) fusion proteins in the baculovirus expression system. Proteins are purified with glutathion Sepharose beads 4B. Basic FlashPlates are coated with 0.1 M sterile filtered sodium bicarbonate, pH 7.6, containing 700 ng of GST-Smad3 per 100 μL. Assay buffer contains 50 mM HEPES (pH 7.4), 5 mM MgCl2, 1 mM CaCl2, 1 mM DTT, 100 mM GTP, 3 μM ATP plus 0.5 μCi/well ɤ33P-ATP, and 85 ng of GST-ALK5 with or without SB 431542. Plates are incubated at 30 °C for 3 hours. The assay buffer is removed by aspiration, and the plate is counted on a Packard TopCount 96-well scintillation plate reader.
Cell Research:[4]
+ Expand
  • Cell lines: MG63 and NIH3T3
  • Concentrations: 0.3 μM
  • Incubation Time: 30 minutes
  • Method: To explore the effects of ligands, MG63 and NIH3T3 cells are seeded at a density of 8 × 104 cells/well in 6-well plates and starved (0.1% FCS for MG63 cells and 0.5% FCS for NIH3T3 cells) for 24 hours before ligand stimulation. Media containing various ligands are exchanged at 48-hours intervals. Cells are trypsinized and counted by a Coulter counter on days 2, 4, and 6 after ligand stimulation. To explore the effects of constitutively active receptors, cells are seeded at a density of 2 × 105 cells/well in 6-well plates. The next day, cells are infected with adenoviruses carrying various cDNAs at a multiplicity of infection of 100. Cells are trypsinized and counted on day 3. Cell proliferation assay is performed in the presence of 0.3 μM SB 431542.
    (Only for Reference)
Animal Research:[6]
+ Expand
  • Animal Models: BALB/c mice receive intraperitoneal (i.p.) injections of colon-26 tumor cells.
  • Formulation: DMSO
  • Dosages: 1 μM solution, 100 μL/mouse
  • Administration: Directly injected into peritoneal cavity
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 76 mg/mL (197.71 mM)
Ethanol 3 mg/mL (7.8 mM)
Water Insoluble
In vivo Add solvents individually and in order:
2% DMSO+30% PEG 300+ddH2O
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 384.39
Formula

C22H16N4O3

CAS No. 301836-41-9
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    I would appreciate it if you can help me in figuring out the formulation for this drug in vivo experiments.

  • Answer:

    S1067 SB431542 in 1% DMSO+30% polyethylene glycol+1% Tween 80 at 30 mg/ml is a suspension for oral gavage. It can also be dissolved in 2% DMSO+30% PEG 300+ddH2O at 5 mg/ml as a clear solution for IP injection.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID