SB431542

Catalog No.S1067

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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SB431542 Chemical Structure

SB431542 Chemical Structure
Molecular Weight: 384.39

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  • Research Area
  • Inhibition Profile
  • SB431542 Mechanism

Product Description

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)
IC50 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
HEK293TNWPYSopKTnWwY4Tpc44hSXO|YYm=MUexNEDPxE1?NXzxeVk5OjJiaB?=NXruemtlTE2VTx?=MVrJcohq[mm2czDUS2JTOiC|aXfuZYxqdmdiaX6gbJVu[W5iSFXLNlk{XCClZXzsd{Bie3Onc4Pl[EBieyCLbnjpZol1cW:wIH;mJHNOSURiYXP0bZZifGmxbjD3bZRpKEmFNUCgc4YhOC5yNkdOwG0>M{ewWFI{OTNyNkK2
H1299MnTwUYloemG2aX;uJGF{e2G7NH[5NFYyKM7:TR?=NEH1ZnMyOi1{NDDoNYKzSno5TE2VTx?=NU\0WYtOUW6mdXPld{BidnSrbXnndoF1d3K7IHHjeIl3cXS7IHHnZYlve3RiaIXtZY4hUDF{OUmgZ4VtdHNiYYPz[ZN{\WRiYYOgTY5pcWKrdHnvckBw\iClZXzsJI1q\3KjdHnvckB4cXSqIFnDOVAhd2ZiMD61{txOM3GwVFI1PDF5NEe5
HaCaTM2j6OGZ2dmO2aX;uJGF{e2G7MlTyN{4zNTVyIN88US=>NXfsUXduOTVibXnuM4nxTGROW09?NF3GZZBKdmirYnn0d{BVT0[kZYThJJJm[2WydH;yJIlvKGi3bXHuJGhiS2GWIHPlcIx{KGG|c3Xzd4VlKGG|IGPtZYQheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkG3Nu69VQ>?Mn;tNlA6OTl4N{i=
HepG2M2OzTGZ2dmO2aX;uJGF{e2G7NETmWnMyOiCqM1Lxb2ROW09?NEj1UHNKdmirYnn0d{BVT0[ULUGgbY4hcHWvYX6gTIVxTzJiY3XscJMh\XiycnXzd4lv\yCSQVmtcJVkcW[ncnHz[UB4cXSqIFnDOVAhd2ZiMD6yOe69VQ>?MYqxPVkyPDB4OB?=
CHO-HIRMlnJSpVv[3Srb36gRZN{[Xl?M4\HSlAvODFvMzFOwG0>MlTyNkBpMnm0SG1UVw>?M1Tjb2lvcGmkaYTzJHRITmKndHGtbY5lfWOnZDDkc5dve3S{ZXHtJJRz[W6|Y4LpdJRqd26jbDDhZ5RqfmG2aX;uJI9nKEGOS{Wg[ZhxemW|c3XkJIlvKEOKTz3ITXIh[2WubIOgZZN{\XO|ZXSgZZMhcW62cnHj[YxtfWyjcjD0doFve2yxY3H0bY9vKG:oIFXHSnAuW22jZEKge4l1cCCLQ{WwJI9nKDBwM{ZOwG0>NVvtRnA5OjRyNUWwOFY>
Sf9M3zDNmZ2dmO2aX;uJGF{e2G7M2XXTFIhcA>?NIfuVmhFVVORM2nkcGlvcGmkaYTzJIh2dWGwIILlZ49u[mmwYX70JGFNUzVicHjvd5Bpd3K7bHH0bY9vKGW6cILld5Nm\CCrbjDT[lkh[2WubIOge4l1cCCLQ{WwJI9nKDFwNUSy{txONEnqc4MyPzV3MkWwOy=>
C32NHTxT4pHfW6ldHnvckBCe3OjeR?=NXf3NHQ4OTBizszNNW\OcpVWOjCqM2LRSmlvcGmkaYTzJHRzgXCjbn;zc41iKGO{dYrpJHkhcW6oZXP0bY9vNWmwZIXj[YQhXEeIYnX0ZUB{cWewYXzpcochcW5ibXnub{BEOzJiY3XscJMh[XRiMUCgeW0>MoDNNVc2OjZ5NUe=
Mouse embryo cardiomyocytesMlLqSpVv[3Srb36gRZN{[Xl?MlHXNVAh|ryPMUWxJIg>NGHocYNKdmirYnn0d{Bqdn[jc3nvckBw\iCWconwZY5we2:vYTDjdpV7cSC\IHnuJI1wfXOnIHXtZpJ6dyClYYLkbY9ugW:leYTld{Bie3Onc4Pl[EBieyCyYYToc4dmdiCrbn\lZ5Rqd25iYYSgNVAhfU1?NVvJV|h4OTd3Mk[3OVc>
Mouse embryo cardiomyocytesM{fBVmZ2dmO2aX;uJGF{e2G7MoLuNVAh|ryPNHizTo8yKGh?MmjnTY5pcWKrdIOgWGdHNWKndHGtNU1qdmS3Y3XkJHNu[WR{IIDoc5NxcG:{eXzheIlwdiCrbjDtc5V{\SCnbXLyfY8h[2G{ZHnvcZlw[3m2ZYOgZZQhOTBidV2=NYjvV3dlOTd3Mk[3OVc>
Mouse embryo cardiomyocytesM{\0cGZ2dmO2aX;uJGF{e2G7NWPLS5A6OTBizszNNEfOTZoyKGh?M2\ZV2lvcGmkaYTzJHRzgXCjbn;zc41iKGO{dYrpJGRuOjiFIHnu[oVkfGmxbj3pcoR2[2WmIGPtZYQzKHCqb4PwbI9zgWyjdHnvckBqdiCvb4Xz[UBmdWK{eX:gZ4Fz\GmxbYnvZ5l1\XNiYYSgNVAhfU1?M1[5c|E4PTJ4N{W3
Trypanosoma cruzi trypomastigotesNUi2S|ZDSW62aX3pZ5Jw[mmjbDDBd5NigQ>?MYKxNEDPxE1?MkPjOEBpMV;JcoR2[2W|IHHueIl1enmyYX7vd49u[WxiYXP0bZZqfHliYXfhbY5{fCCWconwZY5we2:vYTDjdpV7cSC2conwc41ie3SrZ3;0[ZMh[XO|ZYPz[YQh[XNiZX\m[YN1KG:wIIDhdoF{cXSnIH3vdpBpd2yxZ4mgZZQhOTBidV2=MVSxO|UzPjd3Nx?=
Mouse cardiomyocytesNHTOTXlCdnSrbXnjdo9jcWGuIFHzd4F6MXuxNEDPxE1?MlLaOEBpMlTiTY5lfWOnczDhcpRqfHK7cHHuc5NwdWGuIHHjeIl3cXS7IHHnZYlve3RiVIL5dIFvd3OxbXGgZ5J2gmliWTDpckBud3W|ZTDjZZJlcW:veX;jfZRmeyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhcW62cnHj[YxtfWyjcjDhcYF{fGmpb4Tld{BifCBzMDD1US=>M2nDWFE4PTJ4N{W3
Mouse cardiomyocytesMn30RY51cW2rY4LvZolidCCDc4PhfS=>NXHMUoYzOTBizszNM{TaVlk3KGh?NV7lUZZXUW6mdXPld{BidnSrdIL5dIFvd3OxbXHsJIFkfGm4aYT5JIFo[Wmwc4SgWJJ6eGGwb4PvcYEh[3K3enmgXUBqdiCvb4Xz[UBk[XKmaX;tfY9kgXSnczDhd5Nme3OnZDDhd{BKdmirYnn0bY9vKG:oIITyfZBwdWG|dHnnc5RmKHKnbHXhd4Uh[XRiMUCgeW0>NXPBZVN3OTd3Mk[3OVc>
HaCaTMWXGeY5kfGmxbjDBd5NigQ>?NVXXOI5bOC5yNTFOwG0>MlvoNkBpNEfjXVlFVVORMV;Ec4V{KG6xdDDpcohq[mm2IGTHSk1j\XSjIHnu[JVk\WRiQVzLOUBi[3Srdnn0fUBqdiCKYVPhWEBk\WyuczDhd5Nme3OnZDDhd{BxO1SSLXz1Z4ln\XKjc3WgdoVxd3K2ZYKgZYN1cX[rdImgZZQhOC5yNTD1US=>NITRc|gyPzV3MkWwOy=>

... 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]
Features

Protocol(Only for 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 Assay: [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.

Animal Study: [6]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Callahan JF, et al. J Med Chem, 2002, 45(5), 999-1001.

[2] Inman GJ, et al. Mol Pharmacol, 2002, 62(1), 65-74.

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Chemical Information

Download SB431542 SDF
Molecular Weight (MW) 384.39
Formula

C22H16N4O3

CAS No. 301836-41-9
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 77 mg/mL (200.31 mM)
Ethanol 3 mg/mL (7.8 mM)
Water <1 mg/mL
In vivo 2% DMSO+30% PEG 300+ddH2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name 4-(4-(benzo[d][1,3]dioxol-5-yl)-5-(pyridin-2-yl)-1H-imidazol-2-yl)benzamide

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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