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。

SC-514

CAS No. : 354812-17-2

MCE 国际站：SC-514

产品活性：SC-514 是一种选择性 IKK-2 抑制剂 (IC₅₀=11.2 μM)，不抑制其他 IKK 亚型或其他丝氨酸-苏氨酸和酪氨酸激酶。

研究领域：NF-κB

作用靶点：IKK

In Vitro: SC-514 inhibits the native IKK complex or recombinant human IKK-1/IKK-2 heterodimer with IC₅₀s of 6.1±2.2 μM and 2.7±0.7 μM, respectively. IKK-2 inhibition by SC-514 is selective, reversible, and competitive with ATP. SC-514 inhibits transcription of NF-κB-dependent genes in IL-1β-induced rheumatoid arthritis-derived synovial fibroblasts in a dose-dependent manner. SC-514 inhibits all forms of recombinant human IKK-2 including rhIKK-2 homodimer, rhIKK-1/rhIKK-2 heterodimer, as well as the constitutively active form of rhIKK-2 with comparable IC₅₀ values in the 3-12 μM range. To evaluate whether the reactive oxygen species (ROS)-inducing IKKβ inhibitor increases the sensitivity of melanoma cells to nitrosourea. The responses of melanoma cells are first assessed to SC-514/Fotemustine co-treatment. Melanoma cell lines are treated with 50 µM of SC-514 and Fotemustine alone and in combination for 48 h and growth inhibition is assessed. Co-treatment with SC-514 significantly enhances Fotemustine-induced cytotoxicity in all melanoma cell lines tested.

In Vivo: SC-514 is efficacious in an acute model of inflammation, namely LPS-induced serum TNFα production in the rat. SC-514 shows a dose-dependent inhibition of TNFα production, validating IKK-2 as a potential anti-inflammatory drug target in vivo. To obtain in vivo evidence for the implication of SC-514 in the response of cancer cells to Fotemustine, the xenograft mouse model of melanoma is used. Nude mice engrafted with A375 or G361 tumors are treated with vehicle control and 25 mg/kg SC-514 and/or 25 mg/kg Fotemustine daily for 13-15 consecutive days and the tumor behavior is monitored. Fotemustine treatment with SC-514 shows a clear combined effect and reduces the size of tumors in mice.

相关产品：Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  Kinase Inhibitor Library  |  NF-κB Signaling Compound Library  |  Stem Cell Signaling Compound Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Differentiation Inducing Compound Library  |  Pyroptosis Compound Library  |  Targeted Diversity Library  |  Anti-Liver Cancer Compound Library   |  Human Metabolite Library  |  Anti-Prostate Cancer Compound Library  |  Highly Selective Inhibitors Library  |  TBK1/IKKε-IN-4  |  Isophysalin A  |  GS143  |  PS-1145  |  Glabrescone C  |  Ertiprotafib  |  IKK-IN-4  |  Resveratrol  |  NF-κB-IN-1  |  HPN-01  |  BAY32-5915  |  Oxaprozin  |  TBK1/IKKε-IN-1  |  LY2409881  |  Tizoxanide  |  Bay 65-1942 (R form)  |  (Rac)-BAY-985  |  Lucidone  |  IKK 16 hydrochloride  |  (Rac)-PF-184  |  BOT-64  |  Malachite green oxalate  |  AZD3264  |  IKKβ-IN-1  |  PHA 408  |  Resveratrol-d₄  |  GSK319347A

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-13802

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。