2156-56-1

Hazard Information

Chemical Properties

white powder

Brand name

Ceresine (Cypros).

General Description

Sodium dichloroacetate is a mitochondrial pyruvate dehydrogenase kinase (PDK) inhibitor that exhibits potent anti-leukemic activity.

Biological Activity

Inhibitor of mitochondrial pyruvate dehydrogenase kinase (PDK). Shifts pyruvate metabolism from glycolysis and lactate production to glucose oxidation in the mitochondria. Induces mitochondrial-dependent apoptosis and reverses the inhibition/downregulation of K V 1.5 channels in cancer but not normal cells. Decreases tumor growth in vitro and in vivo .

Synthesis

79-43-6

2156-56-1

General procedure for the synthesis of sodium dichloroacetate from dichloroacetic acid: Cl2CHCO2H (135 μL, 1.64 mmol) was dissolved in H2O (2 mL), treated with 1.00 M NaOH (1.60 mL, 1.60 mmol), and the reaction was stirred for 2 hours at room temperature. Upon completion of the reaction, the volatiles were removed under vacuum to give a pale yellow residue. The residue was suspended in acetone, the suspension was filtered, the resulting colorless solid was washed with acetone and finally dried under vacuum. Yield: 227 mg, 96% yield.

storage

Desiccate at RT

References

[1] Journal of Organometallic Chemistry, 2018, vol. 869, p. 201 - 211

Material Safety Data Sheet(MSDS)

Questions And Answer

• Uses

  Sodium dichloroacetate (DCA) is a mitochondrial pyruvate dehydrogenase kinase inhibitor, and is an orally absorbable small molecular compound for MELAS syndrome, and children with congenital lactic acidosis and other diseases that are treated in the clinic. Recent studies had found that DCA acts as a potential vasoprotective agent by inhibiting PDK2 and reducing coronary endarterium proliferation. Further, DCA promotes brain regeneration after cerebral ischemia, which indicates that DCA might play an important role in VD.

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