MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

EMD638683

CAS No. : 1181770-72-8

MCE 国际站：EMD638683

产品活性：EMD638683 是具有高度选择性的 SGK1 抑制剂，IC₅₀ 值为 3 μM。

研究领域：Metabolic Enzyme/Protease

作用靶点：SGK

In Vitro: EMD638683 is a SGK1 inhibitor. EMD638683 inhibits the NDRG1 (N-Myc downstream-regulated gene 1) phosphorylation, an effect requiring 3.35±0.32 μM EMD638683 in the cell culture medium for half maximal effect (IC₅₀). EMD638683 has also an inhibitory effect on cAMP-dependent protein kinase (PKA), mitogen- and stress-activated protein kinase 1 (MSK1), protein kinase C-related kinase 2 (PKR2), and the SGK isoforms SGK2 and SGK3. In both, control and EMD638683 (50 μM)-treated CaCo-2 cells, radiation significantly increases the percentage of CaCo-2 cells undergoing late apoptosis. EMD638683 treatment alone tends to enhance the percentage of apoptotic CaCo-2 cells. Following radiation the percentage of apoptotic EMD638683-treated CaCo-2 cells is significantly higher than the percentage of apoptotic control cells. Thus, EMD638683 treatment significantly augments the apoptosis following radiation.

In Vivo: The colon is significantly longer and the colon weight significantly lower in EMD638683-treated mice than in placebo-treated mice, a finding pointing to an influence of EMD638683 on tumor growth following chemical carcinogenesis. In addition, the stomach weight is significantly lower in the EMD treated group. Most importantly, the number of developing tumors following carcinogenic treatment is significantly blunted by EMD638683 treatment. EMD638683 (20 mg/kg, intragastrically) prevents progression of monocrotaline (MCT)-induced pulmonary vascular remodeling in rats. Hemodynamic characteristics show that EMD638683 treatment attenuates right ventricular systolic pressure (RVSP) (15.8±2.5 vs. 28.2±3.1 mmHg; P<0.05; n=6) and right ventricular hypertrophy index (RVHI) (0.27±0.02 vs. 0.41±0.06;P<0.05; n=6) compare to vehicle-dosed controls.

相关产品：Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Metabolism/Protease Compound Library  |  Anti-Cancer Compound Library  |  Targeted Diversity Library  |  Human Metabolite Library  |  Highly Selective Inhibitors Library  |  SGK1-IN-3  |  Hu7691 free base  |  SI-113  |  CKI-7 free base  |  SGK1-IN-4  |  PF-4950834  |  EMD638683 R-Form  |  HaloPROTAC-E  |  GSK 650394  |  SGK1-IN-1  |  SGK1-IN-2  |  PROTAC SGK3 degrader-1

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

货号: HY-15193

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种全球独家化合物库，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；
•   50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。