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Sodium dichloroacetate
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产品介绍
产品介绍
产品信息
抗原名称
PDK4,PDK2
商品描述
Dichloroacetate, a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress a mitochondrial potassium-ion channel axis, trigger apoptosis in cancer cells, and inhibit tumor growth.
分子量
150.92
纯度
＞98%
可溶性
DMSO ：30 mg/mL (198.78 mM)
Water ：30 mg/mL (198.78 mM)
Water ：30 mg/mL (198.78 mM)
外观
white powder
In vitro(体外研究)
DCA can trigger apoptosis of human lung, breast and brain cancer cells. After DCA treatment, cancer cells shows increased levels of ROS, depolarization of the MMP in vitro and increased apoptosis both in vitro and in vivo. DCA inhibits the activity of pyruvate dehydrogenase kinase (PDK), thereby stimulating the mitochondrial enzyme pyruvate dehydrogenase (PDH). When turned off, PDH no longer converts pyruvate to acetyl-CoA required for mitochondrial respiration and glucose dependent oxidative phosphorylation. DCA thus shifts cellular metabolism from glycolysis to glucose oxidation, decreasing the mitochondrial membrane potential gradient and helping to open mitochondrial transition pores. This metabolic switch facilitates translocation of pro-apoptotic mediators like cytochrome c (cyt c) and apoptosis inducing factor (AIF), both of which stimulate apoptosis. DCA thereby drives cancer cells to commit suicide by apoptosis.
In vivo(体内研究)
DCA can act as a cytostatic agent in vitro and in vivo, without causing apoptosis (programmed cell death). DCA is discovered to be a safe drug with no cardiac, pulmonary, renal or bone marrow toxicity. The most serious common side effect consists of peripheral neuropathy, which is reversible. DCA has anti-cancer activity in several cancer types including colon, prostate, ovarian, neuroblastoma, lung carcinoid, cervical, endometrial, cholangiocarcinoma, sarcoma and T-cell lymphoma. Other antineoplastic actions of DCA have also been suggested. These include angiogenesis blockade, changes in expression of HIF1-α, alteration of pH regulators V-ATPase and MCT1, and other cell survival regulators such as PUMA, GLUT1, Bcl2 and p53. DCA is able to significantly reduce metastatic burden in the lungs of rats in a highly metastatic in vivo model of breast cancer. In vivo the DCA-Na treatment induces 20% survival and decreased the tumoral diameter, volume and weight, without affect the body weight and avoid metastasis in C57BL/6 mice.
背景
别名
二氯乙酸钠；DCA
分子式
C2HCl2NaO2
CAS号
2156-56-1
MDL
MFCD00070489
PK值
pKa: 1.37
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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