SB431542

Catalog No.S1067

For research use only.

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.

SB431542 Chemical Structure

CAS No. 301836-41-9

Selleck's SB431542 has been cited by 451 publications

Purity & Quality Control

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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 NX7RcVM4TnWwY4Tpc44hSXO|YYm= M1zyO|ExKM7:TR?= NFnlNmczOiCq NEXXXpFFVVOR MXPJcohq[mm2czDUS2JTOiC|aXfuZYxqdmdiaX6gbJVu[W5iSFXLNlk{XCClZXzsd{Bie3Onc4Pl[EBieyCLbnjpZol1cW:wIH;mJHNOSURiYXP0bZZifGmxbjD3bZRpKEmFNUCgc4YhOC5yNkdOwG0> MkXsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNzM{C2NlYoRjJ|MUOwOlI3RC:jPh?=
H1299 M3rkcW1q\3KjdHnvckBCe3OjeR?= M{H5R|Eh|ryP M2jQd|EzNTJ2IHi= MmrlSG1UVw>? NFnxS|RKdmS3Y3XzJIFvfGmvaXfyZZRwenliYXP0bZZqfHliYXfhbY5{fCCqdX3hckBJOTJ7OTDj[YxteyCjc4Pld5Nm\CCjczDJcohq[mm2aX;uJI9nKGOnbHygcYloemG2aX;uJJdqfGhiSVO1NEBw\iByLkZOwG0> MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRzN{S3PUc,OjR2MUe0O|k9N2F-
HaCaT Mk[4SpVv[3Srb36gRZN{[Xl? MkjoN{4zNTVyIN88US=> NYr2[nJrOTVibXnu MkTlSG1UVw>? NEPVOnhKdmirYnn0d{BVT0[kZYThJJJm[2WydH;yJIlvKGi3bXHuJGhiS2GWIHPlcIx{KGG|c3Xzd4VlKGG|IGPtZYQheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkG3Nu69VQ>? M3uzT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOUG5Olc5Lz5{MEmxPVY4QDxxYU6=
HepG2 NU\iNWUyTnWwY4Tpc44hSXO|YYm= NG\TeHEyOiCq MXnEUXNQ NUG0cph[UW6qaXLpeJMhXEeIUj2xJIlvKGi3bXHuJGhmeEd{IHPlcIx{KGW6cILld5NqdmdiUFHJMYx2[2moZYLhd4Uhf2m2aDDJR|UxKG:oIECuNlXPxE1? MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTlzNEC2PEc,OTl7MUSwOlg9N2F-
CHO-HIR M3;MemZ2dmO2aX;uJGF{e2G7 M4HVNlAvODFvMzFOwG0> M1TnSFIhcA>? M4foV2ROW09? M1\KZ2lvcGmkaYTzJHRITmKndHGtbY5lfWOnZDDkc5dve3S{ZXHtJJRz[W6|Y4LpdJRqd26jbDDhZ5RqfmG2aX;uJI9nKEGOS{Wg[ZhxemW|c3XkJIlvKEOKTz3ITXIh[2WubIOgZZN{\XO|ZXSgZZMhcW62cnHj[YxtfWyjcjD0doFve2yxY3H0bY9vKG:oIFXHSnAuW22jZEKge4l1cCCLQ{WwJI9nKDBwM{ZOwG0> MkTtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNUWwOFYoRjJ2MEW1NFQ3RC:jPh?=
Sf9 MnLESpVv[3Srb36gRZN{[Xl? NXi3SZN[OiCq M4Pqb2ROW09? Mom3TY5pcWKrdIOgbJVu[W5icnXjc41jcW6jboSgRWxMPSCyaH;zdIhwenmuYYTpc44h\XiycnXzd4VlKGmwIGPmPUBk\WyuczD3bZRpKEmFNUCgc4YhOS53NENOwG0> MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV3MkWwO{c,OTd3NUK1NFc9N2F-
C32 NIfBVG9HfW6ldHnvckBCe3OjeR?= NXzEdmpOOTBizszN MXqyNIg> NWLmZ2NNUW6qaXLpeJMhXHK7cHHuc5NwdWFiY4L1fokhYSCrbn\lZ5Rqd25vaX7keYNm\CCWR1\i[ZRiKHOrZ37hcIlv\yCrbjDtbY5sKEN|MjDj[YxteyCjdDCxNEB2VQ>? M2\ifVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NUK2O|U4Lz5zN{WyOlc2PzxxYU6=
Mouse embryo cardiomyocytes MYnGeY5kfGmxbjDBd5NigQ>? MV2xNEDPxE1? MnLiNUBp NITaR25KdmirYnn0d{Bqdn[jc3nvckBw\iCWconwZY5we2:vYTDjdpV7cSC\IHnuJI1wfXOnIHXtZpJ6dyClYYLkbY9ugW:leYTld{Bie3Onc4Pl[EBieyCyYYToc4dmdiCrbn\lZ5Rqd25iYYSgNVAhfU1? MonqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3Mk[3OVcoRjF5NUK2O|U4RC:jPh?=
Mouse embryo cardiomyocytes MkPRSpVv[3Srb36gRZN{[Xl? MWqxNEDPxE1? M4\zflEhcA>? NITzbG9KdmirYnn0d{BVT0ZvYnX0ZU0yNWmwZIXj[YQhW22jZEKgdIhwe3Cqb4L5cIF1cW:wIHnuJI1wfXOnIHXtZpJ6dyClYYLkbY9ugW:leYTld{BifCBzMDD1US=> Mo\QQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3Mk[3OVcoRjF5NUK2O|U4RC:jPh?=
Mouse embryo cardiomyocytes MlO2SpVv[3Srb36gRZN{[Xl? MkDuNVAh|ryP NVPvVVU3OSCq MoTFTY5pcWKrdIOgWJJ6eGGwb4PvcYEh[3K3enmgSI0zQENiaX7m[YN1cW:wLXnu[JVk\WRiU33h[FIheGixc4Doc5J6dGG2aX;uJIlvKG2xdYPlJIVu[nK7bzDjZZJlcW:veX;jfZRmeyCjdDCxNEB2VQ>? MlfvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3Mk[3OVcoRjF5NUK2O|U4RC:jPh?=
Trypanosoma cruzi trypomastigotes M4PubGFvfGmvaXPyc4Jq[WxiQYPzZZk> MknwNVAh|ryP MVO0JIg> M4jZ[Wlv\HWlZYOgZY51cXS{eYDhco9{d22jbDDhZ5Rqfmm2eTDh[4FqdnO2IGTyfZBidm:|b33hJINzfXqrIITyfZBwdWG|dHnnc5RmeyCjc4Pld5Nm\CCjczDl[oZm[3Rib36gdIFz[XOrdHWgcY9zeGixbH;nfUBifCBzMDD1US=> NYK3W|N4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1NlY4PTdpPkG3OVI3PzV5PD;hQi=>
Mouse cardiomyocytes NXLHfGdOSW62aX3pZ5Jw[mmjbDDBd5NigQ>? MmLXNVAh|ryP NHXQS5A1KGh? NVjESHpQUW6mdXPld{BidnSrdIL5dIFvd3OxbXHsJIFkfGm4aYT5JIFo[Wmwc4SgWJJ6eGGwb4PvcYEh[3K3enmgXUBqdiCvb4Xz[UBk[XKmaX;tfY9kgXSnczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hd2ZiaX70doFk\WyudXzhdkBidWG|dHnnc5RmeyCjdDCxNEB2VQ>? NELCeYQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{WyOlc2Pyd-MUe1NlY4PTd:L3G+
Mouse cardiomyocytes MYHBcpRqdWmlcn;ibYFtKEG|c3H5 NVTRO5ZSOTBizszN MV25OkBp NUjrZllPUW6mdXPld{BidnSrdIL5dIFvd3OxbXHsJIFkfGm4aYT5JIFo[Wmwc4SgWJJ6eGGwb4PvcYEh[3K3enmgXUBqdiCvb4Xz[UBk[XKmaX;tfY9kgXSnczDhd5Nme3OnZDDhd{BKdmirYnn0bY9vKG:oIITyfZBwdWG|dHnnc5RmKHKnbHXhd4Uh[XRiMUCgeW0> M13r[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NUK2O|U4Lz5zN{WyOlc2PzxxYU6=
HaCaT NUPhTnA2TnWwY4Tpc44hSXO|YYm= MofCNE4xPSEQvF2= NHnENGEzKGh? MVrEUXNQ MkLMSI9meyCwb4SgbY5pcWKrdDDUS2Yu[mW2YTDpcoR2[2WmIFHMT|Uh[WO2aY\peJkhcW5iSHHDZXQh[2WubIOgZZN{\XO|ZXSgZZMheDOWUD3seYNq\mW{YYPlJJJmeG:{dHXyJIFkfGm4aYT5JIF1KDBwMEWgeW0> NU\MWGVzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe1OVI2ODdpPkG3OVUzPTB5PD;hQi=>
Assay
Methods Test Index PMID
Western blot phospho-SMAD3 / Phospho-p38 ; Y397 phospho-FAK ; pSmad2 / p-AKT / E-cadherin / vimentin / snail / slug ; CK18 / Fibronectin / Vimentin 17113264 26269769 30134011
Growth inhibition assay Cell viability 28125630
Immunofluorescence Smad2/3 19619490
Immunofluorescence Na+/K+-ATPase 23451286
ELISA collagen 1 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 (from reference)

Kinase Assay: [1]
  • 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]
  • 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]
  • 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.

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 3 years -20°C powder
2 years -80°C in solvent
Smiles C1OC2=C(O1)C=C(C=C2)C3=C(NC(=N3)C4=CC=C(C=C4)C(=O)N)C5=CC=CC=N5

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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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.

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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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