DCA (Sodium dichloroacetate)
别名: Dichloroacetic acid, bichloroacetic acid, BCA 中文名称：二氯乙酸钠
DCA (Sodium dichloroacetate)是 pyruvate dehydrogenase kinase (PDK) 的特异性抑制剂，对PDK2和PDK4的IC50值分别为183和80 μM；可抑制 Na+-K+-2Cl- cotransporter 和线粒体钾离子通道轴。Sodium dichloroacetate 可增加活性氧的生成，引起癌细胞凋亡，并抑制肿瘤生长。
DCA (Sodium dichloroacetate) Chemical Structure
CAS: 2156-56-1
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产品质控
DCA (Sodium dichloroacetate)相关产品
相关信号通路图
Dehydrogenase抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| MCF7 | Function assay | 10 mM | 12 hrs | Inhibition of PDK1 in human MCF7 cells assessed as increase in oxygen consumption rate at 10 mM after 12 hrs | 27006991 |
| MCF7 | Function assay | 10 mM | 12 hrs | Inhibition of PDK1 in human MCF7 cells assessed as decrease in extracellular acidification rate at 10 mM after 12 hrs | 27006991 |
| MCF7 | Function assay | 10 mM | 12 hrs | Inhibition of PDK1 in human MCF7 cells assessed as decrease in proton production rate at 10 mM after 12 hrs | 27006991 |
| MCF7 | Function assay | 10 mM | 12 hrs | Inhibition of PDK1 in human MCF7 cells assessed as increase in ratio of oxygen consumption rate to extracellular acidification rate at 10 mM after 12 hrs | 27006991 |
| MCF7 | Function assay | 10 mM | 12 hrs | Inhibition of PDK1 in human MCF7 cells assessed as decrease in lactate production at 10 mM after 12 hrs | 27006991 |
| NCI-H1975 | Antiproliferative assay | 20 mM | 72 hrs | Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability at 20 mM after 72 hrs by MTT assay | 30470491 |
| MCF7 | Antitumor assay | 30 mg/kg | two weeks | Antitumor activity against human MCF7 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 30 mg/kg, iv administered every two days for two weeks measured after 14 days | 31509699 |
| MCF7 | Function assay | 30 uM | 4 hrs | Induction of metabolic reversal from aerobic glycolysis to oxidative phosphorylation in human MCF7 cells assessed as increase in extracellular acidification rate at 30 uM pretreated for 4 hrs followed by glucose addition after 25 mins by seahorse XF24 ext | 31509699 |
| MCF7 | Function assay | 30 uM | 4 hrs | Induction of metabolic reversal from aerobic glycolysis to oxidative phosphorylation in human MCF7 cells assessed as increase in extracellular acidification rate at 30 uM pretreated for 4 hrs followed by glucose addition after 25 mins followed by subsequent assay | 31509699 |
| MCF7 | Function assay | 30 uM | 4 hrs | Induction of metabolic reversal from aerobic glycolysis to oxidative phosphorylation in human MCF7 cells assessed as decline in extracellular acidification rate at 30 uM pretreated for 4 hrs followed by glucose addition after 25 mins followed by subsequent assay | 31509699 |
| MCF7 | Function assay | 30 uM | 6 hrs | Induction of metabolic reversal from aerobic glycolysis to oxidative phosphorylation in human MCF7 cells assessed as decrease in oxygen consumption rate at 30 uM pretreated for 6 hrs followed by oligomycin A addition after 25 mins followed by subsequent assay | 31509699 |
| MCF7 | Function assay | 90 mins | Inhibition of PDK1 (unknown origin) expressed in human MCF7 cells using PDK tide as substrate measured after 90 mins in presence of ATP by ADP-Glo luminescent kinase assay | 31509699 | |
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | DCA (Sodium dichloroacetate)是 pyruvate dehydrogenase kinase (PDK) 的特异性抑制剂，对PDK2和PDK4的IC50值分别为183和80 μM；可抑制 Na+-K+-2Cl- cotransporter 和线粒体钾离子通道轴。Sodium dichloroacetate 可增加活性氧的生成，引起癌细胞凋亡，并抑制肿瘤生长。 | ||||
|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | DCA可引起人类肺部、乳腺和脑癌细胞的凋亡[1]。经DCA处理后，癌细胞中的ROS水平升高、MMP去极化、在体内外都能够增加凋亡[2]。DCA抑制丙酮酸脱氢酶激酶（PDK）的活性，因而刺激线粒体丙酮酸脱氢酶（PDH）。当PDH处于关闭状态时，PDH不再将丙酮酸转化为acetyl-CoA（线粒体呼吸和葡萄糖依赖的氧化磷酸化过程所必需）。从而，DCA将细胞代谢从糖酵解转换为葡萄糖氧化，降低线粒体膜电位，促进线粒体转运孔的开放。这一系列代谢转换有助于促凋亡介质如cyt c和AIF的易位。因而，DCA可通过凋亡反应驱动癌细胞自杀[3]。 | |||
|---|---|---|---|---|
| 细胞实验 | 细胞系 | 乳腺癌细胞 | ||
| 浓度 | 5 mM | |||
| 孵育时间 | 24-72 h | |||
| 方法 | 将细胞以3000细胞/孔的密度铺于96孔板。用DCA和ATO处理24-72小时，然后换成新鲜的含30 μg/ml的中性红培养基孵育3小时。PBS洗涤细胞，加入lysis buffer(acetic acid/methanol, 80%/20%)，在540 nm处检测吸光值。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | pPDH E1α / PDH E1α |
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25630799 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | DCA在体内体外可作为细胞生长抑制剂，而不引起程序性细胞死亡（凋亡）。DCA是一种安全性较高的药物，没有心脏、肺部、肾脏或骨髓毒性。最为严重的副作用包括周围神经病变，该作用为可逆过程。DCA在好几种癌症类型中，包括结肠癌、前列腺癌、卵巢癌、成神经细胞瘤、肺癌、子宫颈癌、子宫内膜、胆管癌、肉瘤和T细胞淋巴瘤具有抗癌活性。DCA的其他一些抗肿瘤作用也被报导，包括阻碍血管生成、改变HIF-1α的表达、pH调节剂V-ATPase和MCT1的改变、其他细胞生存调节子如PUMA、GLUT1、Bcl2和p53的改变。在大鼠高转移乳腺癌模型中，DCA能够显著地减少肺部转移性负担[1]。在C57BL/6小鼠中，DCA-Na的体内给药可诱导20%的生存率提高并减少肿瘤直径、体积和重量，而不影响其体重、并避免转移[3]。 | |
|---|---|---|
| 动物实验 | Animal Models | C57BL/6 mice |
| Dosages | 500 and 1000 mg/kg | |
| Administration | i.p. | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06073106 | Not yet recruiting | Stroke|Traumatic Brain Injury|Knee Osteoarthritis|Breast Cancer |
Tan Tock Seng Hospital|Rehabilitation Research Institute of Singapore (RRIS)|Woodlands Health (WH) |
December 2023 | -- |
| NCT05810623 | Not yet recruiting | Upper Urinary Tract Urothelial Carcinoma|Bladder Cancer |
David D''Andrea|Medical University of Vienna |
June 1 2023 | Phase 3 |
| NCT05646485 | Recruiting | Bladder Cancer|Urothelial Carcinoma|Hematuria|Smoking Cessation |
University of Texas Southwestern Medical Center |
May 5 2023 | Not Applicable |
| NCT05460533 | Recruiting | B-cell Acute Lymphoblastic Leukemia |
Memorial Sloan Kettering Cancer Center|Novartis Pharmaceuticals |
July 12 2022 | Phase 2 |
化学信息&溶解度
| 分子量 | 150.92 | 分子式 | C2HCl2O2.Na |
| CAS号 | 2156-56-1 | SDF | Download DCA (Sodium dichloroacetate) SDF |
| Smiles | C(C(=O)[O-])(Cl)Cl.[Na+] | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
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摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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