- ￥193 - 5864
- TargetMol
- T6337
- 2026年07月07日
2 年钻石会员
企业认证
相关产品推荐更多 >
万千商家帮你免费找货
0 人在求购买到急需产品
- 详细信息
- 文献和实验
- 技术资料
- CAS号：
446859-33-2
- 规格：
1mLx10mM(inDMSO)/1mg/2mg/5mg/10mg/25mg/50mg/100mg/500mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥446.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥193.0 |
| 规格： | 2mg | 产品价格： | ￥253.0 |
| 规格： | 5mg | 产品价格： | ￥397.0 |
| 规格： | 10mg | 产品价格： | ￥596.0 |
| 规格： | 25mg | 产品价格： | ￥1144.0 |
| 规格： | 50mg | 产品价格： | ￥1696.0 |
| 规格： | 100mg | 产品价格： | ￥2520.0 |
| 规格： | 500mg | 产品价格： | ￥5864.0 |
Product Introduction
Bioactivity
| 名称 | RepSox |
| 描述 | RepSox (ALK5 Inhibitor II) is a TGFβR-1/ALK5 inhibitor that selectively inhibits the binding of ATP to ALK5 and the autophosphorylation of ALK5 (IC50=23/4 nM). RepSox induces adipogenesis in MEFs cells. |
| 细胞实验 | RepSox is dissolved in DMSO and stored, and then diluted with appropriate media (DMSO 1%) before use[1]. To test anti-TGF-β activity of compounds, HepG2 cells are seeded in 96 well microplates at a concentration of 35000 cells per well in 200 μL of serum-containing medium. The microplates are then placed for 24 h in a cell incubator at 37°C, 5% CO2 atm. RepSox dissolved in DMSO are then added at concentrations of 50 nM to 10 μM (final concentration of DMSO 1%) for 30 min prior to the addition of recombinant TGF-β (1 ng/mL). After an overnight incubation, the cells are washed with PBS and lysed by addition of 10 μL of passive lysis buffer. Inhibition of luciferase activity relative to control groups is used as a measure of compound activity. A concentration?response curve is constructed from which an IC50 value is determined graphically[1]. |
| 激酶实验 | The kinase domain of ALK5 is cloned by PCR and expressed in a baculovirus/Sf9 cells system. The protein is 6-His tagged in the C terminus and purified by affinity chromatography using a Ni2+column, and the obtained material is used to assess compound activity in an autophosphorylation assay. Purified enzyme (10 nM) is incubated in 50 μL of Tris buffer (Tris 50 mM, pH 7.4; NaCl, 100 mM; MgCl2, 5 mM; MnCl2, 5 mM; and DTT, 10 mM). The enzyme is preincubated with different concentrations of RepSox (0.1% DMSO final concentration in the test) for 10 min at 37°C. The reaction is then initiated by the addition of 3 μM ATP (0.5 μCi γ-33P-ATP). After 15 min at 37°C, phosphorylation is stopped by the addition of SDS?PAGE sample buffer (50 mM Tris-HCl, pH 6.9, 2.5% glycerol, 1% SDS, and 5% β-mercaptoethanol). The samples are boiled for 5 min at 95°C and run on a 12% SDS?PAGE. Dried gels are exposed to a phosphor screen overnight. ALK5 autophosphorylation is quantified using a Storm imaging system[1]. |
| 体外活性 | 方法：小鼠胚胎成纤维细胞 MEFs 用 RepSox (10 µM) 处理 10 天，使用 oil red O 染色检测细胞脂肪。 结果：RepSox 处理的 MEFs 中出现了许多脂肪细胞样细胞，脂滴的 oil red O 染色证实了脂肪细胞分化。[1] 方法：绵羊成纤维细胞用 RepSox (10-25 nM) 处理 3 天，使用显微镜观察细胞形态。 结果：在 RepSox 处理三天后，绵羊成纤维细胞获得了显著不同的形态，并从纺锤形转变为具有更多聚束的细长形状。[2] |
| 体内活性 | 方法：为检测对肠内神经胶质细胞 EGCs 分化的影响，将 RepSox (3-10 mg/kg in 0.5% CMC-Na) 腹腔注射给 GFAP-Cre:Rosa26-tdTomato 小鼠，每天一次，持续两周。 结果：RepSox 可以促进 EGCs 转化为神经元，并改善体内胃肠道运动。[3] 方法：为检测体内抗肿瘤活性，将 RepSox (5-20 mg/kg) 腹腔注射携带骨肉瘤 143B 的 nude 小鼠模型，每两天一次，持续三周。 结果：RepSox 有效地抑制了骨肉瘤的生长，并且在裸鼠中具有低毒性。[4] |
| 存储条件 | Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (17.4 mM), Sonication is recommended. Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 51 mg/mL (177.5 mM), Sonication is recommended. |
| 关键字 | Transforming growth factor beta receptors | TGFβR1 | TGF-β/Smad | TGF-β Receptor | TGFβ | TGFbeta/Smad | TGF-beta | TGFbeta | TGF-b/Smad | TGFb | Smad | SJN-2511 | SJN2511 | RepSox | Inhibitor | inhibit | E616452 | E 616452 | ALK5 |
| 相关产品 | Trimethylamine N-oxide | Pirfenidone | Crizotinib | Melamine | A 83-01 | SB-431542 | Alectinib | Cetrimonium bromide | Galunisertib | Alantolactone | Brigatinib | Hydrochlorothiazide |
| 相关库 | Inhibitor Library | Angiogenesis related Compound Library | Anti-Breast Cancer Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | Cytokine Inhibitor Library | Kinase Inhibitor Library | Stem Cell Differentiation Compound Library | TGF-beta/Smad Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Human Metabolite Library |
风险提示：丁香通仅作为第三方平台，为商家信息发布提供平台空间。用户咨询产品时请注意保护个人信息及财产安全，合理判断，谨慎选购商品，商家和用户对交易行为负责。对于医疗器械类产品，请先查证核实企业经营资质和医疗器械产品注册证情况。
文献和实验该产品被引用文献
官网有文献
相关实验
网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
技术资料暂无技术资料 索取技术资料
文献支持
化合物 RepSox【446859-33-2】
￥193 - 5864
