For research use only.

Catalog No.S1067

284 publications

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.

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Selleck's SB431542 has been cited by 284 publications

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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.
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 M2Gxd2Z2dmO2aX;uJGF{e2G7 NFv4SZkyOCEQvF2= MnTpNlIhcA>? MXrEUXNQ NF7TdVNKdmirYnn0d{BVT0KUMjDzbYdv[WyrbnegbY4hcHWvYX6gTGVMOjl|VDDj[YxteyCjc4Pld5Nm\CCjczDJcohq[mm2aX;uJI9nKFOPQVSgZYN1cX[jdHnvckB4cXSqIFnDOVAhd2ZiMD6wOlbPxE1? NIW2elEzOzF|ME[yOi=>
H1299 M4DE[W1q\3KjdHnvckBCe3OjeR?= NFmxTJoyKM7:TR?= NHTyVnMyOi1{NDDo MYjEUXNQ M1;lSGlv\HWlZYOgZY51cW2rZ4LheI9zgSCjY4Tpeol1gSCjZ3HpcpN1KGi3bXHuJGgyOjl7IHPlcIx{KGG|c3Xzd4VlKGG|IFnubIljcXSrb36gc4Yh[2WubDDtbYdz[XSrb36ge4l1cCCLQ{WwJI9nKDBwNd88US=> M4KzZlI1PDF5NEe5
HaCaT MWTGeY5kfGmxbjDBd5NigQ>? NX75TlltOy5{LUWwJO69VQ>? MXqxOUBucW5? Mle1SG1UVw>? Ml;wTY5pcWKrdIOgWGdH[mW2YTDy[YNmeHSxcjDpckBpfW2jbjDIZWNiXCClZXzsd{Bie3Onc4Pl[EBieyCVbXHkJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5zN{NOwG0> NHfpbYozODlzOU[3PC=>
HepG2 NYO4OZZTTnWwY4Tpc44hSXO|YYm= NFvXclMyOiCq M2XYOWROW09? Mn;QTY5pcWKrdIOgWGdHWi1zIHnuJIh2dWGwIFjldGczKGOnbHzzJIV5eHKnc4PpcochWEGLLXz1Z4ln\XKjc3Wge4l1cCCLQ{WwJI9nKDBwMkZOwG0> NFHkTJkyQTlzNEC2PC=>
CHO-HIR NIX5eZpHfW6ldHnvckBCe3OjeR?= MWmwMlAyNTNizszN NFP3S24zKGh? MV3EUXNQ NF3hS41KdmirYnn0d{BVT0[kZYThMYlv\HWlZXSg[I94dnO2cnXhcUB1emGwc3PybZB1cW:wYXygZYN1cX[jdHnvckBw\iCDTFu1JIV5eHKnc4Pl[EBqdiCFSF:tTGlTKGOnbHzzJIF{e2W|c3XkJIF{KGmwdILhZ4VtdHWuYYKgeJJidnOub3PheIlwdiCxZjDFS2ZRNVOvYXSyJJdqfGhiSVO1NEBw\iByLkO1{txO NWGxTYc{OjRyNUWwOFY>
Sf9 NGLjV5BHfW6ldHnvckBCe3OjeR?= MlSwNkBp NX70cnBnTE2VTx?= NGXDfGhKdmirYnn0d{BpfW2jbjDy[YNwdWKrbnHueEBCVEt3IIDoc5NxcG:{eXzheIlwdiCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJJdqfGhiSVO1NEBw\iBzLkW0Nu69VQ>? MlPONVc2PTJ3MEe=
C32 M{fwT2Z2dmO2aX;uJGF{e2G7 NYGzUWlwOTBizszN NVj5S3I3OjCq MlezTY5pcWKrdIOgWJJ6eGGwb4PvcYEh[3K3enmgXUBqdm[nY4Tpc44ucW6mdXPl[EBVT0[kZYThJJNq\26jbHnu[{BqdiCvaX7rJGM{OiClZXzsd{BifCBzMDD1US=> MYCxO|UzPjd3Nx?=
Mouse embryo cardiomyocytes NEnTV5hHfW6ldHnvckBCe3OjeR?= MnG5NVAh|ryP M2\2Z|EhcA>? NWWzVG1nUW6qaXLpeJMhcW64YYPpc44hd2ZiVIL5dIFvd3OxbXGgZ5J2gmliWTDpckBud3W|ZTDlcYJzgW9iY3Hy[IlwdXmxY4n0[ZMh[XO|ZYPz[YQh[XNicHH0bI9o\W5iaX7m[YN1cW:wIHH0JFExKHWP Mkn6NVc2OjZ5NUe=
Mouse embryo cardiomyocytes NFL2VW5HfW6ldHnvckBCe3OjeR?= M3vt[|ExKM7:TR?= NILkSXIyKGh? NWO3T4hVUW6qaXLpeJMhXEeILXLleIEuOS2rbnT1Z4VlKFOvYXSyJJBpd3OyaH;yfYxifGmxbjDpckBud3W|ZTDlcYJzgW9iY3Hy[IlwdXmxY4n0[ZMh[XRiMUCgeW0> MVKxO|UzPjd3Nx?=
Mouse embryo cardiomyocytes M1vMc2Z2dmO2aX;uJGF{e2G7 NYTpPG5iOTBizszN NULTVHg2OSCq MkfoTY5pcWKrdIOgWJJ6eGGwb4PvcYEh[3K3enmgSI0zQENiaX7m[YN1cW:wLXnu[JVk\WRiU33h[FIheGixc4Doc5J6dGG2aX;uJIlvKG2xdYPlJIVu[nK7bzDjZZJlcW:veX;jfZRmeyCjdDCxNEB2VQ>? NVzGWXg5OTd3Mk[3OVc>
Trypanosoma cruzi trypomastigotes NFz1NHNCdnSrbXnjdo9jcWGuIFHzd4F6 Ml;ZNVAh|ryP MlHaOEBp NEPI[ZhKdmS3Y3XzJIFvfGm2conwZY5we2:vYXygZYN1cX[rdImgZYdicW6|dDDUdplx[W6xc3;tZUBkenW8aTD0dplxd22jc4Tp[491\XNiYYPz[ZN{\WRiYYOg[YZn\WO2IH;uJJBiemG|aYTlJI1wenCqb3zv[5kh[XRiMUCgeW0> MYGxO|UzPjd3Nx?=
Mouse cardiomyocytes NV6wT3U3SW62aX3pZ5Jw[mmjbDDBd5NigQ>? NVT6cWRROTBizszN M4nyOlQhcA>? M4fiNmlv\HWlZYOgZY51cXS{eYDhco9{d22jbDDhZ5Rqfmm2eTDh[4FqdnO2IGTyfZBidm:|b33hJINzfXqrIGmgbY4hdW:3c3WgZ4Fz\GmxbYnvZ5l1\XNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKGmwdILhZ4VtdHWuYYKgZY1ie3SrZ3;0[ZMh[XRiMUCgeW0> M1;zdlE4PTJ4N{W3
Mouse cardiomyocytes MYDBcpRqdWmlcn;ibYFtKEG|c3H5 M3\ZS|ExKM7:TR?= MojEPVYhcA>? MoTWTY5lfWOnczDhcpRqfHK7cHHuc5NwdWGuIHHjeIl3cXS7IHHnZYlve3RiVIL5dIFvd3OxbXGgZ5J2gmliWTDpckBud3W|ZTDjZZJlcW:veX;jfZRmeyCjc4Pld5Nm\CCjczDJcohq[mm2aX;uJI9nKHS{eYDvcYF{fGmpb4TlJJJmdGWjc3WgZZQhOTBidV2= M2TKXlE4PTJ4N{W3
HaCaT M2HGbmZ2dmO2aX;uJGF{e2G7 MX:wMlA2KM7:TR?= MmrMNkBp NIHZdFJFVVOR NF72ZWRFd2W|IH7veEBqdmirYnn0JHRITi2kZYThJIlv\HWlZXSgRWxMPSCjY4Tpeol1gSCrbjDIZWNiXCClZXzsd{Bie3Onc4Pl[EBieyCyM2TQMYx2[2moZYLhd4UhemWyb4L0[ZIh[WO2aY\peJkh[XRiMD6wOUB2VQ>? NHLFTGcyPzV3MkWwOy=>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
phospho-SMAD3 / Phospho-p38 ; 

PubMed: 17113264     

Quiescent IMR-90 cells were treated with/without TGF-β1 (2 ng/ml) in the presence or absence of increasing concentrations of the TGF-βR1(ALK5) inhibitor, SB431542. Cell lysates were collected after 45 min and assessed by SDS-PAGE followed by western immunoblotting for phospho-SMAD3 and phospho-p38 MAPK. The blots were then striped and probed for total SMAD3 and p38 MAPK, respectively.

Y397 phospho-FAK; 

PubMed: 17113264     

Quiescent IMR-90 cells were treated with TGF-β1 (2 ng/ml) in the presence/absence of the p38 MAPK inhibitor, SB203580 (6 μM). Cell lysates collected after 16 h were assessed for Y397-phosphorylated FAK by SDS-PAGE and western immunoblotting. Blots were stripped and probed for total FAK.

pSmad2 / p-AKT / E-cadherin / vimentin / snail / slug; 

PubMed: 26269769     

B16-pldMock cells and B16-pldNodal cells were treating with SB431542 (10 mM) in a time dependent manner, and then the protein was collected for Western blotting analysis.

CK18 / Fibronectin / Vimentin; 

PubMed: 30134011     

Representative Western blots (upper panel) and densitometric analysis (lower panel) for E‐cadherin, CK18 (epithelial markers), fibronectin and vimentin (mesenchymal markers) normalized to β-actin in HepG2 and BEL7402 cells with or without SB431542 treatment in CM and HBSS.

17113264 26269769 30134011
Growth inhibition assay
Cell viability; 

PubMed: 28125630     

Cells were treated with 1 mg/L, 4 mg/L, and 16 mg/L of fluoride with or without 10μmol/L SB431542 for 4 and 7 days. MTT assay was used to detect cell viability. Absorbance was measured at 490 nm in aspectrophotometer. Average optical density (OD) value of cells viability was represented as mean±SD (n = 8) (*P < 0.05, **P < 0.01 compare with control group; aa P< 0.05, compare with SB431542 group).


PubMed: 19619490     

MEFs were treated with 25 mM glucose, TGF-β or glucose and SB431542 for 30 min, and the subcellular localization of Smad2/3 was visualized. DAPI was used to stain the nuclei.


PubMed: 23451286     

Blocking the TGF-receptor signaling by SB431542 enabled the subcellular localization of Na+/K+-ATPase and ZO-1 at the plasma membrane. Scale bar: 100 μm.

collagen 1; 

PubMed: 23451286     

ELISA assay revealed that SB431542 significantly downregulated the secretion of type I collagen to the culture supernatant. **P<0.05.

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]


Kinase Assay: [1]
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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]
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  • 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]
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  • Animal Models: BALB/c mice receive intraperitoneal (i.p.) injections of colon-26 tumor cells.
  • 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 to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.

* 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


CAS No. 301836-41-9
Storage powder
in solvent
Synonyms N/A
Smiles C1OC2=C(O1)C=C(C=C2)C3=C(NC(=N3)C4=CC=C(C=C4)C(=O)N)C5=CC=CC=N5

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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