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。
TAK-243
CAS No. : 1450833-55-2
MCE 国际站:TAK-243
产品活性:TAK-243 (MLN7243) 是一种首创的,选择性的泛素激活酶,UAE (UBA1) 抑制剂 (IC50=1 nM),其阻断了泛素结合,破坏了单泛素信号传导和全蛋白泛素化。TAK-243 (MLN7243) 诱导内质网应激 (ERS) 反应,消除 NF-κB 通路活化,促进细胞凋亡。
研究领域:Metabolic Enzyme/Protease | NF-κB | Apoptosis
作用靶点:E1/E2/E3 Enzyme | NF-κB | Apoptosis
In Vitro: TAK-243 shows anti-proliferative effect on a panel of cell lines derived from hematologic and solid tumors with variable EC50 values that ranged from 0.006 μM to 1.31 μM.
?TAK-243 reduces growth and viability of human AML cell lines (OCI-AML2, TEX, U937 and NB4) in a concentration- and time-dependent manner with IC50s ranging from 15-40 nM after treatment for 48 hours.
In Vivo: TAK-243 significantly delays tumor growth in mice (T/C=0.02) with no toxicity as evidenced by no changes in mouse body weight, serum chemistry, or organ histology. TAK-243 reduces primary AML tumor burden in both tested samples without toxicity.
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Apoptosis Compound Library | Immunology/Inflammation Compound Library | Metabolism/Protease Compound Library | NF-κB Signaling Compound Library | Stem Cell Signaling Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Anti-Aging Compound Library | Antioxidant Compound Library | Differentiation Inducing Compound Library | Oxygen Sensing Compound Library | Ubiquitination Compound Library | Endoplasmic Reticulum Stress Compound Library | Pyroptosis Compound Library | Chemical Probe Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Anti-Obesity Compound Library | Transcription Factor-Targeted Library | Anti-Liver Cancer Compound Library | Antidepressant Compound Library | Anti-Prostate Cancer Compound Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Pain-Related Compound Library | Metabolic Enzyme Compound Library | Highly Selective Inhibitors Library | Highly Selective Activators Library | Cell Death Library | Anti-Hematopathy Compound Library | Anti-Ovarian Cancer Compound Library | Multi-Target Compound Library | Radioprotector Library | Mitophagy Compound Library | Bioactive Compound Library Max | MG-132 | Phorbol 12-myristate 13-acetate | Doxorubicin hydrochloride | Bafilomycin A1 | Tamoxifen | Y-27632 | Paclitaxel | Z-VAD-FMK | LY294002 | 2-Deoxy-D-glucose | Angiotensin II human | Acetylcysteine | Staurosporine | Actinomycin D | SB-431542 | 5-Fluorouracil | Bortezomib | Oxaliplatin | Deferoxamine mesylate | Sorafenib | Trametinib | Gemcitabine | Temozolomide | Etoposide | Rotenone | Mdivi-1 | Monomethyl auristatin E | Decitabine | Ruxolitinib | Elesclomol
热门产品线:重组蛋白 | 药物筛选 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Dye Reagents | PROTAC | Isotope-Labeled Compounds
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域;
• 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。