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. : 72926-24-0
MCE 国际站:K858 (Racemic)
产品活性:K858 Racemic 是一种 ATP 非竞争性的驱动蛋白 Eg5 抑制剂,IC50 值为 1.3 μM。
研究领域:Cell Cycle/DNA Damage | Cytoskeleton | Apoptosis
作用靶点:Kinesin | Apoptosis
In Vitro: K858 Racemic is an ATP-uncompetitive inhibitor of Eg5 with an IC50 of 1.3 μM. K858 does not inhibit the ATPase activity of the mitotic kinesins CENP-E and MKLP1, or the conventional kinesin heavy chain even at 200 μM. K858 induces mitotic arrest and growth inhibition via the activation of the Mad2-mediated spindle checkpoint. K858 (5 μM) induces mitotic cell death in cancer cells but not in normal cells. K858 (1, 10, 100 μM) inhibits the MCF7, BT474 and SKBR3 cell lines, and only at 10 and 100 μM suppresses MDA-MB231 cell line after treatment for 24 h. K858 incereases Bax/Bcl2 RNA ratio and survivin in the four cell lines. Furthermore, the up-regulation of survivin is totally reversed by wortmannin (phosphoinositide 3-kinase AKT) in MCF7 cells.
In Vivo: K858 (50, 150 mg/kg, p.o.) shows antitumor activity in an A2780 ovarian cancer xenograft model, also inhibits tumor grwoth in a HCT116 colon cancer xenograft model via 100 mg/kg twice a day orally for 5 days. K858 (100 mg/kg, p.o., qd ×5) displays no neurotoxic side effects in mice.
相关产品:Bioactive Compound Library Plus | Apoptosis Compound Library | Cell Cycle/DNA Damage Compound Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Cytoskeleton Compound Library | Targeted Diversity Library | Pain-Related Compound Library | Highly Selective Inhibitors Library | Highly Selective Activators Library | SY-5609 | BRD4 Inhibitor-18 | 8α-Tigloyloxyhirsutinolide 13-O-acetate | AAPK-25 | Dutasteride-13C6 | Oleic acid-13C | Anticancer agent 120 | Abacavir sulfate | Meloxicam-d3-1 | Thailanstatin D | SB-218078 | Toyocamycin | Sorafenib-d4 | Busulfan | PTC-028 | Dinaciclib | CR-1-31-B | 142I5 | Farudodstat | Ecteinascidin 770 | Filanesib TFA | AT9283 | Staurosporine | SNS-032 | AZA1 | Antitumor agent-96 | Bleomycin A5 | Xevinapant | Mangiferin | Cambinol
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。