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受注：045-509-1970 |
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化学情報
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C22H16N4O3 |
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| 分子量 | 384.39 | CAS No. | 301836-41-9 | |
| Solubility (25°C)* | 体外 | DMSO | 77 mg/mL (200.31 mM) | |
| Ethanol | 77 mg/mL (200.31 mM) | |||
| Water | Insoluble | |||
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* <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. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | SB431542 は強力かつ選択的 ALK5 阻害剤であり、cell-free assay における IC50 は 94 nM です。p38 MAPK などのキナーゼよりも ALK5 に対して 100 倍の選択性を有しています。 |
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| 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] |
| 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] |
プロトコル(参考用のみ)
| キナーゼアッセイ | Flashplate assay for ALK5 | |
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| 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. | ||
| 細胞アッセイ | 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. | |
| 動物実験 | 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 | |
参考
カスタマーフィードバック
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Data from [Acta Biomater, 2014, 10(7):3108-16]
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Data from [Development, 2013, 140, 660-666]
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Data from [Stem Cells Dev, 2013]
Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：
| Small extracellular vesicles derived from human induced pluripotent stem cell-differentiated neural progenitor cells mitigate retinal ganglion cell degeneration in a mouse model of optic nerve injury [ Neural Regen Res, 2025, 20(2):587-597] | PubMed: 38819069 |
| WNT signalling control by KDM5C during development affects cognition [ Nature, 2024, 627(8004):594-603] | PubMed: 38383780 |
| WNT signalling control by KDM5C during development affects cognition [ Nature, 2024, 10.1038/s41586-024-07067-y] | PubMed: 38383780 |
| The extracellular matrix integrates mitochondrial homeostasis [ Cell, 2024, S0092-8674(24)00638-X] | PubMed: 38942015 |
| Generation of complex bone marrow organoids from human induced pluripotent stem cells [ Nat Methods, 2024, 10.1038/s41592-024-02172-2] | PubMed: 38374263 |
| Long-term engrafting multilineage hematopoietic cells differentiated from human induced pluripotent stem cells [ Nat Biotechnol, 2024, 10.1038/s41587-024-02360-7] | PubMed: 39223325 |
| Osteopontin drives neuroinflammation and cell loss in MAPT-N279K frontotemporal dementia patient neurons [ Cell Stem Cell, 2024, S1934-5909(24)00094-8] | PubMed: 38626772 |
| Retinoic acid induces human gastruloids with posterior embryo-like structures [ Nat Cell Biol, 2024, 10.1038/s41556-024-01487-8] | PubMed: 39164488 |
| Reassessment of marker genes in human induced pluripotent stem cells for enhanced quality control [ Nat Commun, 2024, 15(1):8547] | PubMed: 39358374 |
| In vitro induction of patterned branchial arch-like aggregate from human pluripotent stem cells [ Nat Commun, 2024, 15(1):1351] | PubMed: 38355589 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。