Powder: -20°C for 3 years | In solvent: -80°C for 2 years
SB 431542 是ALK5/TGF-β type I Receptor 的选择性抑制剂,其IC50=94 nM。
产品描述 | SB-431542 is a potent and selective inhibitor of ALK5 (IC50: 94 nM) and is also an inhibitor of ALK4 (IC50: 140 nM) and ALK7. |
靶点活性 | ALK5:94 nM, ALK4:140 nM |
体外活性 | SB-431542 inhibits TGF-beta1-induced fibronectin mRNA formation while displaying no measurable cytotoxicity in the 48 h XTT assay [1]. SB-431542 (1 μM) significantly reduced the TGFβ–induced nuclear accumulation of Smad proteins. The IC50 for inhibiting TGFβ–induced nuclear fluorescence is approximately 50 nM. BMP-stimulated Smad1 nuclear fluorescence in MG63 cells was unaffected by SB-431542 [2]. the synergistic action of two inhibitors of SMAD signaling, Noggin and SB431542, is sufficient to induce rapid and complete neural conversion of >80% of hES cells under adherent culture conditions [3]. |
体内活性 | SB-431542 augmented the capacity of bone marrow dendritic cells (BM-DCs) and human DCs to incorporate FITC-conjugated dextran. Intraperitoneal administration of SB-431542 initiated 3 and 7 days after the implantation of colon-26 cancer cells into the peritoneal cavity of BALB/c mice significantly induced CTL activity against colon-26 [4]. SB-431542 significantly inhibited lung metastasis from transplanted 4T1 mammary tumors in Balb/c mice [5]. |
激酶实验 | Kinase assays were performed with 65 nM GSTALK5 and 184 nM GST-Smad3 in 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 1 mM dithiothreitol, and 3 M ATP. Reactions were incubated with 0.5 μCi of [33P]γATP for 3 h at 30°C. Phosphorylated protein was captured on P-81 paper, washed with 0.5% phosphoric acid, and counted by liquid scintillation. Alternatively, Smad3 or Smad1 protein was also coated onto FlashPlate Sterile Basic Microplates. Kinase assays were then performed in FlashPlates with same assay conditions using either the kinase domain of ALK5 with Smad3 as a substrate or the kinase domain of ALK6 (BMP receptor) with Smad1 as substrate. Plates were washed three times with phosphate buffer and counted by TopCount [2]. |
细胞实验 | A498 cells were seeded at 5,000 to 10,000 cells/well in 96-well plates. The cells were serum-deprived for 24 h and then treated with compounds for 48 h to assess the cellular toxicity. Cell viability is determined by incubating cells for 4 h with XTT labeling and electron coupling reagent. Live cells with active mitochondria produce an orange-colored product, formazan, which is detected using a plate reader at between A450 nm and A500 nm with a reference wavelength greater than 600 nm. The absorbance values correlate with the number of viable cells [2]. |
动物实验 | BALB/c mice received intraperitoneal (i.p.) injections of colon-26 tumor cells. Three days after tumor cell inoculation, SB-431542 (1 μM solution, 100 μl/animal) or vehicle alone was directly injected into the peritoneal cavity. CTL activities were measured by a standard 4 h 51Cr release assay after culturing spleen cells with γ-irradiated tumor cells for five days in the absence of added growth factors. In vitro experiments, cell lysate of HLA-A*2402 positive gastric cancer cell line, OCUM-8, was incubated with human DC cultures for 4 h. After washing extensively, PBMCs obtained from the same volunteer as DCs were incubated for 7 days and measured CTL activity by 51Cr release assay. NK activity was tested using 51Cr release assay against K562 [4]. |
别名 | SB 431542, 4-[4-(1,3-苯并二唑-5-基)-5-(2-吡啶基)-1H-咪唑-2-基]-苯酰胺水合物 |
分子量 | 384.39 |
分子式 | C22H16N4O3 |
CAS No. | 301836-41-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
DMSO: 38.4 mg/mL (100 mM)
Ethanol: 3.8 mg/mL (10 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
SB-431542 301836-41-9 Angiogenesis Stem Cells Tyrosine Kinase/Adaptors ALK TGF-beta/Smad SB 431542 Transforming growth factor beta receptors inhibit 4-[4-(1,3-苯并二唑-5-基)-5-(2-吡啶基)-1H-咪唑-2-基]-苯酰胺水合物 TGF-β Receptor SB431542 Inhibitor inhibitor