SB431542

製品コード: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化学構造

CAS No. 301836-41-9

サイズ 価格(税別)
10mM (1mL in DMSO) JPY 25700
JPY 20200
JPY 80000
JPY 212800

代表番号: 03-5615-9297|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(501)

製品安全説明書

TGF-beta/Smad阻害剤の選択性比較

相関TGF-beta/Smad製品

生物活性

製品説明 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.
ターゲット
ALK4 [2]
(Cell-free assay)
ALK7 [2]
(Cell-free assay)
ALK5 [1]
(Cell-free assay)
94 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293T MnziSpVv[3Srb36gRZN{[Xl? MkWwNVAh|ryP M{XTXlIzKGh? M4fQcmROW09? MkTHTY5pcWKrdIOgWGdDWjJic3nncoFtcW6pIHnuJIh2dWGwIFjFT|I6O1RiY3XscJMh[XO|ZYPz[YQh[XNiSX7obYJqfGmxbjDv[kBUVUGGIHHjeIl3[XSrb36ge4l1cCCLQ{WwJI9nKDBwME[2{txO NXrCXGpLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOxN|A3OjZpPkKzNVMxPjJ4PD;hQi=>
H1299 M4f4Vm1q\3KjdHnvckBCe3OjeR?= MYqxJO69VQ>? NEKw[IoyOi1{NDDo NHrLdGVFVVOR MXzJcoR2[2W|IHHueIlucWe{YYTvdpkh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDINVI6QSClZXzsd{Bie3Onc4Pl[EBieyCLbnjpZol1cW:wIH;mJINmdGxibXnndoF1cW:wIIfpeIghUUN3MDDv[kAxNjYQvF2= M33DTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEG3OFc6Lz5{NESxO|Q4QTxxYU6=
HaCaT M1nIZmZ2dmO2aX;uJGF{e2G7 Mm\4N{4zNTVyIN88US=> MoLHNVUhdWmw NInYSHpFVVOR NGTVOlFKdmirYnn0d{BVT0[kZYThJJJm[2WydH;yJIlvKGi3bXHuJGhiS2GWIHPlcIx{KGG|c3Xzd4VlKGG|IGPtZYQheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkG3Nu69VQ>? NXfOTlRTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC5NVk3PzhpPkKwPVE6Pjd6PD;hQi=>
HepG2 MXPGeY5kfGmxbjDBd5NigQ>? NYfQeWl2OTJiaB?= MXXEUXNQ M3PDWWlvcGmkaYTzJHRITlJvMTDpckBpfW2jbjDI[ZBIOiClZXzsd{BmgHC{ZYPzbY5oKFCDST3seYNq\mW{YYPlJJdqfGhiSVO1NEBw\iByLkK1{txO MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTlzNEC2PEc,OTl7MUSwOlg9N2F-
CHO-HIR M1P2PWZ2dmO2aX;uJGF{e2G7 MXewMlAyNTNizszN NIjjN4MzKGh? MXLEUXNQ M1zjVWlvcGmkaYTzJHRITmKndHGtbY5lfWOnZDDkc5dve3S{ZXHtJJRz[W6|Y4LpdJRqd26jbDDhZ5RqfmG2aX;uJI9nKEGOS{Wg[ZhxemW|c3XkJIlvKEOKTz3ITXIh[2WubIOgZZN{\XO|ZXSgZZMhcW62cnHj[YxtfWyjcjD0doFve2yxY3H0bY9vKG:oIFXHSnAuW22jZEKge4l1cCCLQ{WwJI9nKDBwM{ZOwG0> NV;YXItLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOVUxPDZpPkK0NFU2ODR4PD;hQi=>
Sf9 MYDGeY5kfGmxbjDBd5NigQ>? NYPQU4hzOiCq NGTiRmVFVVOR MWjJcohq[mm2czDoeY1idiC{ZXPvcYJqdmGwdDDBUGs2KHCqb4PwbI9zgWyjdHnvckBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IIfpeIghUUN3MDDv[kAyNjV2Mt88US=> MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV3MkWwO{c,OTd3NUK1NFc9N2F-
C32 MnnFSpVv[3Srb36gRZN{[Xl? MlPJNVAh|ryP NXTUOVVPOjCq NGPRelNKdmirYnn0d{BVenmyYX7vd49u[SClcoX6bUB[KGmwZnXjeIlwdi2rbnT1Z4VlKFSJRnLleIEhe2mpbnHsbY5oKGmwIH3pcoshSzN{IHPlcIx{KGG2IEGwJJVO MoTBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3Mk[3OVcoRjF5NUK2O|U4RC:jPh?=
Mouse embryo cardiomyocytes MlrrSpVv[3Srb36gRZN{[Xl? MlL4NVAh|ryP NYfxVZZNOSCq M1vkOmlvcGmkaYTzJIlvfmG|aX;uJI9nKFS{eYDhco9{d22jIHPyeZpqKFliaX6gcY92e2ViZX3idplwKGOjcnTpc416d2O7dHXzJIF{e2W|c3XkJIF{KHCjdHjv[4VvKGmwZnXjeIlwdiCjdDCxNEB2VQ>? MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV{Nke1O{c,OTd3Mk[3OVc9N2F-
Mouse embryo cardiomyocytes Ml7HSpVv[3Srb36gRZN{[Xl? M{noZlExKM7:TR?= M2TiZVEhcA>? M1TkfWlvcGmkaYTzJHRITi2kZYThMVEucW6mdXPl[EBUdWGmMjDwbI9{eGixconsZZRqd25iaX6gcY92e2ViZX3idplwKGOjcnTpc416d2O7dHXzJIF1KDFyIIXN NI\tZ4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{WyOlc2Pyd-MUe1NlY4PTd:L3G+
Mouse embryo cardiomyocytes Mo[0SpVv[3Srb36gRZN{[Xl? MXexNEDPxE1? MWixJIg> M1HudWlvcGmkaYTzJHRzgXCjbn;zc41iKGO{dYrpJGRuOjiFIHnu[oVkfGmxbj3pcoR2[2WmIGPtZYQzKHCqb4PwbI9zgWyjdHnvckBqdiCvb4Xz[UBmdWK{eX:gZ4Fz\GmxbYnvZ5l1\XNiYYSgNVAhfU1? Mlz5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3Mk[3OVcoRjF5NUK2O|U4RC:jPh?=
Trypanosoma cruzi trypomastigotes MmDsRY51cW2rY4LvZolidCCDc4PhfS=> NGnHV20yOCEQvF2= NGnaSmc1KGh? NH\NfZVKdmS3Y3XzJIFvfGm2conwZY5we2:vYXygZYN1cX[rdImgZYdicW6|dDDUdplx[W6xc3;tZUBkenW8aTD0dplxd22jc4Tp[491\XNiYYPz[ZN{\WRiYYOg[YZn\WO2IH;uJJBiemG|aYTlJI1wenCqb3zv[5kh[XRiMUCgeW0> NEHaZVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{WyOlc2Pyd-MUe1NlY4PTd:L3G+
Mouse cardiomyocytes MlXlRY51cW2rY4LvZolidCCDc4PhfS=> M1P6[|ExKM7:TR?= MXy0JIg> NVvobnhZUW6mdXPld{BidnSrdIL5dIFvd3OxbXHsJIFkfGm4aYT5JIFo[Wmwc4SgWJJ6eGGwb4PvcYEh[3K3enmgXUBqdiCvb4Xz[UBk[XKmaX;tfY9kgXSnczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hd2ZiaX70doFk\WyudXzhdkBidWG|dHnnc5RmeyCjdDCxNEB2VQ>? M3zZTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NUK2O|U4Lz5zN{WyOlc2PzxxYU6=
Mouse cardiomyocytes M3XMUmFvfGmvaXPyc4Jq[WxiQYPzZZk> MnrjNVAh|ryP Mlf5PVYhcA>? Ml;XTY5lfWOnczDhcpRqfHK7cHHuc5NwdWGuIHHjeIl3cXS7IHHnZYlve3RiVIL5dIFvd3OxbXGgZ5J2gmliWTDpckBud3W|ZTDjZZJlcW:veX;jfZRmeyCjc4Pld5Nm\CCjczDJcohq[mm2aX;uJI9nKHS{eYDvcYF{fGmpb4TlJJJmdGWjc3WgZZQhOTBidV2= M3T5[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NUK2O|U4Lz5zN{WyOlc2PzxxYU6=
HaCaT MVzGeY5kfGmxbjDBd5NigQ>? MVqwMlA2KM7:TR?= MVSyJIg> NGrQUIxFVVOR NYnIcJlITG:nczDuc5QhcW6qaXLpeEBVT0ZvYnX0ZUBqdmS3Y3XkJGFNUzViYXP0bZZqfHliaX6gTIFE[VRiY3XscJMh[XO|ZYPz[YQh[XNicEPUVE1tfWOrZnXyZZNmKHKncH;yeIVzKGGldHn2bZR6KGG2IECuNFUhfU1? MmXNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3NUK1NFcoRjF5NUWyOVA4RC:jPh?=
アッセイ
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
体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験: [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.

細胞試験:[4]
  • 細胞株:MG63 and NIH3T3
  • 濃度: 0.3 μM
  • 反応時間:30 minutes
  • 実験の流れ: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.
動物試験:[6]
  • 動物モデル:BALB/c mice receive intraperitoneal (i.p.) injections of colon-26 tumor cells.
  • 投薬量:1 μM solution, 100 μL/mouse
  • 投与方法:Directly injected into peritoneal cavity

溶解度 (25°C)

体外

体内

左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+30% PEG 300+ddH2O
混合させたのち直ちに使用することを推奨します。

5mg/mL

化学情報

分子量 384.39
化学式

C22H16N4O3

CAS No. 301836-41-9
Storage 3年 -20°C
2年 -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

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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質量 濃度 体積 分子量

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よくある質問(FAQ)

質問1:
I would appreciate it if you can help me in figuring out the formulation for this drug in vivo experiments.

回答
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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