化合物 SB 431542|T1726|TargetMol

SB-431542
301836-41-9

￥412 5mg 起订

￥667 10mg 起订

￥2530 50mg 起订

上海更新日期：2024-09-23

TargetMol中国（陶术生物）

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产品详情:

中文名称：: 化合物 SB 431542

英文名称：: SB-431542

CAS号：: 301836-41-9

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.87%

产品类别：: 抑制剂

货号：: T1726

Product Introduction

Bioactivity

名称	SB-431542
描述	SB-431542 is an inhibitor of ALK5/TGF-β type I Receptor (IC50=94 nM) and is selective. SB 431542 also has inhibitory activity against ALK4 and ALK7 but not other proteins. SB 431542 can be used for induced differentiation of stem cells.
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].
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].
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].
体外活性	方法：人肾细胞 293T、人类结肠癌来源的非致瘤性细胞 FET 和人肺腺癌细胞 A549 用 SB-431542 (2-10 μM) 和 TGF-β1 (12.5 ng/mL) 处理 1 h，使用 Western Blot 方法检测靶点蛋白表达水平。结果：TGF-β1 诱导了 Smad2/3 和 Smad4 之间的复合物形成。SB-431542 以剂量依赖的方式，通过阻断 TGF-β 诱导的磷酸化和Smad2/3的激活，阻断复合物形成。[1] 方法：人胶质母细胞瘤细胞 D54MG 用 SB-431542 (1-10 μM) 处理 24 h，使用 Transwell 方法检测细胞迁移情况。结果： SB-431542抑制 TGF-βRI 信号传导以浓度依赖的方式阻断 D54MG 细胞的细胞迁移。[2] 方法：人多能干细胞 hESCs 用含 SB-431542 (10 nM) 和 Noggin (500 ng/mL) 的 KSR 培养基培养 11 天，使用 Immunofluorescence 方法检测细胞分化情况。结果：神经诱导通过 PAX6 的表达来监测，PAX6 是神经直肠真皮分化的早期标志物。与单独使用 Noggin 或 SB-431542 时不到 10% 的 PAX6+ 细胞相比，用 Noggin 和 SB-431542 联合处理显著提高了神经诱导的效率，使其超过总细胞的 80%。[3]
体内活性	方法：为检测体内抗肿瘤活性，将 SB-431542 (10 mg/kg in 20% DMSO/80% corn oil) 腹腔注射给携带小鼠乳腺癌肿瘤 4T1 的 Balb/c 小鼠，每周三次，持续四周。结果：SB-431542 可显著抑制 4T1 乳腺肿瘤的肺转移。[4] 方法：为研究肌腱损伤的治疗方法，将 SB-431542 (10 mg/kg) 腹腔注射给大面积肩袖撕裂的 C57B/6J 小鼠模型，每天一次，持续二或六周。结果：SB-431542 抑制 TGF-β1 信号传导可减少纤维化、脂肪浸润和肌肉重量减轻。SB-431542 治疗通过促进纤维/脂肪生成祖细胞 (FAP) 的凋亡，减少了损伤肌肉中 FAP 的数量，FAP 是肩袖肌纤维化和脂肪浸润的重要细胞来源。[5]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 16.67 mg/mL (43.36 mM) 10% DMSO+90% Saline : 0.1 mg/mL (0.26 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. Ethanol : 3.8 mg/mL (10 mM)
关键字	Transforming growth factor beta receptors \| inhibit \| TGF-β Receptor \| SB431542 \| SB-431542 \| Inhibitor
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相关库	抑制剂库 \| 血管生成库 \| 抗癌活性化合物库 \| 经典已知活性库 \| 已知活性化合物库 \| 激酶抑制剂库 \| 高选择性抑制剂库 \| TGF-β/Smad靶点化合物库 \| 膜蛋白靶向化合物库 \| 酪氨酸激酶分子库

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|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

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