VLX600
规格
Cas Number | 327031-55-0 |
规格或纯度 | 10mM in DMSO |
包装 | 1ml |
产品信息
品牌 | 阿拉丁 |
浓度 | 10mM in DMSO |
简短描述 | OXPHOS 抑制剂 |
英文简短描述 | OXPHOS Inhibitors |
过滤标签 | Compound libraries |
储存温度 | -80℃储存 |
运输条件 | 超低温冰袋运输 |
生化和生理学机理 | VLX600 是一种新型氧化磷酸化(OXPHOS)铁螯合抑制剂,能以协同方式增强肿瘤球体内的辐射效应。在营养饥饿条件下,VLX600 显示出更强的细胞毒性活性。VLX600 可诱导自噬和线粒体抑制,并具有抗肿瘤活性。 |
英文描述 |
Information VLX600 VLX600 is a novel iron-chelating inhibitor of oxidative phosphorylation (OXPHOS) , potentiates the effect of radiation in tumor spheroids in a synergistic manner. VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation. VLX600 induces autophagy and mitochondrial inhibition with antitumor activity. Targets OXPHOS In vitro VLX600 shows enhanced cytotoxic activity under conditions of nutrient starvation. Mitochondrial inhibition with VLX600 has a direct antitumor effect in vitro while appearing to promote glycolysis through increased AKT signaling and glucose transporter expression. When combined with imatinib, VLX600 prevents imatinib-induced cell cycle escape and reduces p27 expression, leading to increased apoptosis when compared to imatinib alone. In vivo VLX600 induces the formation of autolysosomes in vivo. VLX600 displays tumour growth inhibition in vivo. When combined with imatinib, VLX600 reduces p27 expression and prevents imatinib-induced cell cycle escape, likely potentiating the antitumoral effects of Kit inhibition. Cell Research(from reference) Cell lines:human GIST-T1 cell line, human HG129 cell line, human GIST-882 cell line, Concentrations:2 μM, 6 μM, 12 μM Incubation Time:48–72h |