型号:_ML282
产品价格:电议      采购度:1904      原产地:中国大陆
发布时间:2020/7/14 15:21:12 所属地区:上海 上海市
简要描述:
CID-1067700 (ML282) 是 pan GTPase 抑制剂,可竞争性抑制大脑 7 (Rab7) 中的 Ras 相关蛋白,Ki 为 13 nM。
标签:ML282
产品详情
MCE 的所有产品仅用作科学研究,我们不为任何个人用途提供产品和服务。
CAS No. : 314042-01-8
MCE 站:CID-1067700
产品活性:CID-1067700 (ML282) 是 pan GTPase 抑制剂,可竞争性抑制大脑 7 (Rab7) 中的 Ras 相关蛋白,Ki 为 13 nM。
研究领域:GPCR/G Protein
作用靶点:Ras
In Vitro: CID-1067700 (ML282) is a pan GTPase inhibitor, and competitively inhibits Rab7 with a Ki of 13 nM. CID-1067700 shows inhibitory activity against nucleotide binding by Rab7, with Kds of 100 nM and 40 nM for BODIPY-GTP and BODIPY-GDP, respectively. With increasing concentration, CID-1067700 causes strong inhibition on binding of the BODIPY-linked nucleotides, with EC50 values of 11.22 ± 1.34 nM for BODIPY-GTP and 20.96 ± 1.34 nM for BODIPY-GDP and calculated Ki values of 12.89 nM and 19.70 nM respectively. CID-1067700 (10 μM) has no effect on the rate of release of bound BODIPY-linked nucleotide by wild type Rab7 under equilibrium binding conditions. CID-1067700 (0-40 μM) inhibits Rab7 activity, NF-κB activation as well as AID induction in B cells. Furthermore, CID-1067700 binds Rab7 with a high affinity (EC50: 10-20 nM), and blocks Class switch DNA recombination (CSR) in B cells via targeting Rab7.
In Vivo: CID-1067700 (ML282; 16 mg/kg, i.p.) prevents disease development in lupus-prone mice by Rab7 inhibition, and reduces IgG-IC deposition in MRL/Faslpr/lpr mice. CID-1067700 also targets B cells and specifically impairs the CSR machinery in vivo.
相关产品:GPCR/G Protein Compound Library | Glutamine Metabolism Compound Library | Ferroptosis Compound Library | Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | AMG-510 | ARS-1620 | NSC 23766 trihydrochloride | BI-2852 | MRTX-1257 | MRTX849 | Pan-RAS-IN-1 | Rhosin hydrochloride | ARS-853 | BAY-293 | ML141 | Salirasib | BI-3406 | EHT 1864 | CASIN | EHop-016 | 1A-116 | ZCL278 | GGTI298 | CCG-1423 | Y16 | MBQ-167 | K-Ras(G12C) inhibitor 12 | PROTAC K-Ras Degrader-1 | CCG-203971 | Kobe0065 | ML-098 | CCG-222740
品牌介绍:
• MCE (MedChemExpress) 拥有数百种全球独家化合物,我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物;
• 10,000 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域;
• 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 等多种期刊及制药收录了MCE客户的科研成果;
• 专业团队跟踪*新的制药及生命科学研究进展,为您提供全球*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。
更新时间:2024/1/2 10:11:10
留言咨询
温馨提示
1.遵守中华人民共和国有关法律、法规,尊重网上道德,承担一切因您的行为而直接或间接引起的法律责任。
2.请您真实的反映产品的情况,不要捏造、诬蔑、造谣。如对产品有任何疑问,也可以留言咨询。
3.未经本站同意,任何人不得利用本留言簿发布个人或团体的具有广告性质的信息或类似言论。
相关新闻
相关产品