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.

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In DMSO USD 143 In stock
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USD 470 In stock
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Cited by 52 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.
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 NVXkWopvTnWwY4Tpc44hSXO|YYm= NWT1d5g2OTBizszN NVrUT4lbOjJiaB?= M1rQdWROW09? MVjJcohq[mm2czDUS2JTOiC|aXfuZYxqdmdiaX6gbJVu[W5iSFXLNlk{XCClZXzsd{Bie3Onc4Pl[EBieyCLbnjpZol1cW:wIH;mJHNOSURiYXP0bZZifGmxbjD3bZRpKEmFNUCgc4YhOC5yNkdOwG0> NFvVTIgzOzF|ME[yOi=>
H1299 M4HDPG1q\3KjdHnvckBCe3OjeR?= M2\3eVEh|ryP NWPhTnRqOTJvMkSgbC=> NGXuUIVFVVOR NIDyeYtKdmS3Y3XzJIFvfGmvaXfyZZRwenliYXP0bZZqfHliYXfhbY5{fCCqdX3hckBJOTJ7OTDj[YxteyCjc4Pld5Nm\CCjczDJcohq[mm2aX;uJI9nKGOnbHygcYloemG2aX;uJJdqfGhiSVO1NEBw\iByLkZOwG0> MkfVNlQ1OTd2N{m=
HaCaT MnjQSpVv[3Srb36gRZN{[Xl? NG\WRno{NjJvNUCg{txO MlmyNVUhdWmw NYO1bXZiTE2VTx?= NGHQXndKdmirYnn0d{BVT0[kZYThJJJm[2WydH;yJIlvKGi3bXHuJGhiS2GWIHPlcIx{KGG|c3Xzd4VlKGG|IGPtZYQheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkG3Nu69VQ>? MkLxNlA6OTl4N{i=
HepG2 NH7vPGVHfW6ldHnvckBCe3OjeR?= MX[xNkBp NWLvcVl6TE2VTx?= MoPHTY5pcWKrdIOgWGdHWi1zIHnuJIh2dWGwIFjldGczKGOnbHzzJIV5eHKnc4PpcochWEGLLXz1Z4ln\XKjc3Wge4l1cCCLQ{WwJI9nKDBwMkZOwG0> M3vIdVE6QTF2ME[4
CHO-HIR MXXGeY5kfGmxbjDBd5NigQ>? MVWwMlAyNTNizszN NHTjTHkzKGh? NFjkboNFVVOR NE\FTlhKdmirYnn0d{BVT0[kZYThMYlv\HWlZXSg[I94dnO2cnXhcUB1emGwc3PybZB1cW:wYXygZYN1cX[jdHnvckBw\iCDTFu1JIV5eHKnc4Pl[EBqdiCFSF:tTGlTKGOnbHzzJIF{e2W|c3XkJIF{KGmwdILhZ4VtdHWuYYKgeJJidnOub3PheIlwdiCxZjDFS2ZRNVOvYXSyJJdqfGhiSVO1NEBw\iByLkO1{txO NGDKb5gzPDB3NUC0Oi=>
Sf9 MX3GeY5kfGmxbjDBd5NigQ>? M3jidlIhcA>? NGrBRXZFVVOR MkTjTY5pcWKrdIOgbJVu[W5icnXjc41jcW6jboSgRWxMPSCyaH;zdIhwenmuYYTpc44h\XiycnXzd4VlKGmwIGPmPUBk\WyuczD3bZRpKEmFNUCgc4YhOS53NENOwG0> M1K1[FE4PTV{NUC3
C32 MmHwSpVv[3Srb36gRZN{[Xl? MUexNEDPxE1? MmXjNlBp NEXKT21KdmirYnn0d{BVenmyYX7vd49u[SClcoX6bUB[KGmwZnXjeIlwdi2rbnT1Z4VlKFSJRnLleIEhe2mpbnHsbY5oKGmwIH3pcoshSzN{IHPlcIx{KGG2IEGwJJVO NWDPXZZCOTd3Mk[3OVc>
Mouse embryo cardiomyocytes M1;FOGZ2dmO2aX;uJGF{e2G7 NVLwcFl1OTBizszN NFvHZ3UyKGh? MYjJcohq[mm2czDpcpZie2mxbjDv[kBVenmyYX7vd49u[SClcoX6bUB[KGmwIH3veZNmKGWvYoL5c{Bk[XKmaX;tfY9kgXSnczDhd5Nme3OnZDDhd{Bx[XSqb3flckBqdm[nY4Tpc44h[XRiMUCgeW0> MkDmNVc2OjZ5NUe=
Mouse embryo cardiomyocytes M{npXmZ2dmO2aX;uJGF{e2G7 M4fJVVExKM7:TR?= NUDNPIE5OSCq M1:5emlvcGmkaYTzJHRITi2kZYThMVEucW6mdXPl[EBUdWGmMjDwbI9{eGixconsZZRqd25iaX6gcY92e2ViZX3idplwKGOjcnTpc416d2O7dHXzJIF1KDFyIIXN MWGxO|UzPjd3Nx?=
Mouse embryo cardiomyocytes NYSwUWN1TnWwY4Tpc44hSXO|YYm= NIXPSIgyOCEQvF2= NH;MNIoyKGh? NI\GbXpKdmirYnn0d{BVenmyYX7vd49u[SClcoX6bUBFdTJ6QzDpcoZm[3Srb36tbY5lfWOnZDDTcYFlOiCyaH;zdIhwenmuYYTpc44hcW5ibX;1d4Uh\W2kconvJINiemSrb335c4N6fGW|IHH0JFExKHWP M1[2clE4PTJ4N{W3
Trypanosoma cruzi trypomastigotes NH7aUJpCdnSrbXnjdo9jcWGuIFHzd4F6 NFXoOVkyOCEQvF2= MnTJOEBp NG[3VIRKdmS3Y3XzJIFvfGm2conwZY5we2:vYXygZYN1cX[rdImgZYdicW6|dDDUdplx[W6xc3;tZUBkenW8aTD0dplxd22jc4Tp[491\XNiYYPz[ZN{\WRiYYOg[YZn\WO2IH;uJJBiemG|aYTlJI1wenCqb3zv[5kh[XRiMUCgeW0> MoLDNVc2OjZ5NUe=
Mouse cardiomyocytes Mm\XRY51cW2rY4LvZolidCCDc4PhfS=> NXjUc4w5OTBizszN M1\XfVQhcA>? NWPU[4FlUW6mdXPld{BidnSrdIL5dIFvd3OxbXHsJIFkfGm4aYT5JIFo[Wmwc4SgWJJ6eGGwb4PvcYEh[3K3enmgXUBqdiCvb4Xz[UBk[XKmaX;tfY9kgXSnczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hd2ZiaX70doFk\WyudXzhdkBidWG|dHnnc5RmeyCjdDCxNEB2VQ>? MknRNVc2OjZ5NUe=
Mouse cardiomyocytes NGi4RmVCdnSrbXnjdo9jcWGuIFHzd4F6 Mk[5NVAh|ryP M2Lielk3KGh? NXTHe5RTUW6mdXPld{BidnSrdIL5dIFvd3OxbXHsJIFkfGm4aYT5JIFo[Wmwc4SgWJJ6eGGwb4PvcYEh[3K3enmgXUBqdiCvb4Xz[UBk[XKmaX;tfY9kgXSnczDhd5Nme3OnZDDhd{BKdmirYnn0bY9vKG:oIITyfZBwdWG|dHnnc5RmKHKnbHXhd4Uh[XRiMUCgeW0> NV3tWHU4OTd3Mk[3OVc>
HaCaT M2niOmZ2dmO2aX;uJGF{e2G7 MnPHNE4xPSEQvF2= MnvuNkBp MoLHSG1UVw>? MUnEc4V{KG6xdDDpcohq[mm2IGTHSk1j\XSjIHnu[JVk\WRiQVzLOUBi[3Srdnn0fUBqdiCKYVPhWEBk\WyuczDhd5Nme3OnZDDhd{BxO1SSLXz1Z4ln\XKjc3WgdoVxd3K2ZYKgZYN1cX[rdImgZZQhOC5yNTD1US=> MmPINVc2PTJ3MEe=

... Click to View More Cell Line Experimental Data

Assay
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).

28125630
Immunofluorescence
Smad2/3; 

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.

19619490
Immunofluorescence
Na+/K+-ATPase; 

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.

23451286
ELISA
collagen 1; 

PubMed: 23451286     


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

23451286
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 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.
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
in solvent
Synonyms N/A

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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.

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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