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。
CAS No. : 874146-69-7
MCE 国际站:PK11007
产品活性:PK11007 是具有抗癌活性的温和硫醇烷基化剂。PK11007 通过两个表面暴露的半胱氨酸的选择性烷基化来稳定 p53,而不影响其 DNA 结合活性。PK11007 通过增加活性氧 (ROS) 水平诱导突变的 p53 癌细胞死亡。
研究领域:Apoptosis | Metabolic Enzyme/Protease | Immunology/Inflammation | NF-κB
作用靶点:MDM-2/p53 | Reactive Oxygen Species
In Vitro: PK11007 (0-120 µM; 24 hours; four p53 wild-type cell lines and fours p53 mutant cell lines) treatment results in a large viability reduction in mutant p53 cell lines MKN1 (V143A), HUH-7 (Y220C), NUGC-3 (Y220C), and SW480 (R273H/P309S) at concentrations ranging from 15 to 30 µM. PK11007 induces mainly caspase-independent cell death.
PK11007 (0-60 µM; 3 hours or 6 hours; NUGC-4, NUGC-3, MKN1, HUH-6, and HUH-7 cancer cells) treatment up-regulates protein levels of the p53 target genes p21, MDM2, and PUMA in a mostly concentration-dependent manner in NUGC-3 (p53-Y220C), HUH-7 (p53-Y220C) and MKN1 (p53-V143A) cells, suggesting partial restoration of transcriptional activity to destabilized p53 mutants. PK11007 also increases p53 activity in HUH-6 and NUGC-4 cells, as indicated by the increase of MDM2, PUMA, and p21 protein levels.
PK11007 (15-20 µM; 4.5 hours or 6 hours; MKN1, HUH-7, NUGC-3, HUH-6 cells) treatment increases transcription of p53 target genes in three mutant p53 cell lines after 6-h treatment. PUMA and p21 mRNA levels are up-regulated by a factor of 2 upon treatment of NUGC-3, MKN, and HUH-7 cells, as well as NOXA for the latter two. MDM2 levels are halved in MKN1 and NUGC-3 cells.
PK11007 viability reduction is potentiated by glutathione depletion. To test whether PK11007 also increases ROS levels, NUGC-3, NUGC-4, HUH-6, HUH-7, and MKN1 cells with PK11007 are incubated for 2 h. There are elevated ROS levels in all cell lines after 2 h. In the mutant p53 cells MKN1, HUH-7, and NUGC-3, however, the ROS increase is higher at 60 µM PK11007 than in NUGC-4 and HUH-6 cells, suggesting that the higher PK11007 sensitivity of the mutant p53 cell lines is mediated by a stronger ROS induction. Basal and PK11007-induced ROS levels in MKN1 cells are at least twofold higher than in other cell lines.
PK11007 inhibits cell proliferation, induces apoptosis and alters genes involved in cell death are all consistent with the ability of PK11007 to reactivate mutant p53.
相关产品: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 | Autophagy Compound Library | Anti-Aging Compound Library | Antioxidant Compound Library | Oxygen Sensing Compound Library | Ferroptosis Compound Library | Pyroptosis Compound Library | Glutamine Metabolism Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Mitochondria-Targeted Compound Library | Transcription Factor-Targeted Library | Anti-Colorectal Cancer Compound Library | Heterocyclic Compound Library | Highly Selective Activators Library | D-α-Hydroxyglutaric acid disodium | 8α-Tigloyloxyhirsutinolide 13-O-acetate | Anticancer agent 120 | 7-Hydroxy-4-methyl-2(1H)-quinolone | N-tert-Butyl-α-phenylnitrone-d14 | BDP 581/591 NHS ester | Cysteamine-d4 hydrochloride | L-Ascorbic acid sodium salt | p53 (17-26) | Manganese(salen) chloride | p53 and MDM2 proteins-interaction-inhibitor (racemic) | Hydroxyphenyl Fluorescein | Navtemadlin | Glucosamine sulfate | Maresin 1 | Antitumor agent-60 | Berberine | 1,3-Dicaffeoylquinic acid | Ciprofloxacin | Echinocystic acid | Lacto-N-fucopentaose I | Nisoldipine-d6 | Arg-Tyr | Roslin 2 bromide | HKPerox-2 | Amifostine trihydrate | 3-Indolepropionic acid | 2-Methoxyestradiol-13C,d3 | MX69 | ADH-6 TFA
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
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。