化合物 RepSox|T6337

RepSox
446859-33-2

￥222 1mg 起订

￥297 2mg 起订

￥497 5mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 化合物 RepSox

英文名称：: RepSox

CAS号：: 446859-33-2

品牌：: TargetMol

产地：: 美国

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

纯度规格：: 99.62%

产品类别：: 抑制剂

货号：: T6337

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.
溶解度	Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 15 mg/mL (52.21 mM), Sonication is recommended.
关键字	TGF-β Receptor \| E 616452 \| E616452 \| RepSox \| SJN2511 \| Transforming growth factor beta receptors \| SJN-2511 \| Inhibitor \| inhibit
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相关库	抑制剂库 \| 血管生成库 \| 经典已知活性库 \| 已知活性化合物库 \| 激酶抑制剂库 \| 抗肝癌化合物库 \| 癌细胞分化化合物库 \| 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

SJN 2511|||E-616452|||ALK5 Inhibitor II|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

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子