AdipoGen Life Sciences

Dichloroacetate [DCA] . sodium salt

CHF 55.00
In stock
AG-CR1-3684-G0011 gCHF 55.00
More Information
Product Details
Synonyms Dichloroacetic acid sodium salt; Bichloroacetic acid; BCA
Product Type Chemical
Properties
Formula

C2HCl2O2 . Na

MW 127.9 . 23.0
CAS 2156-56-1
Purity Chemicals ≥98%
Appearance White to off-white solid.
Solubility Soluble in water (10mg/ml) or DMSO (10mg/ml).
InChi Key LUPNKHXLFSSUGS-UHFFFAOYSA-M
Smiles ClC(Cl)C([O-])=O.[Na+]
Shipping and Handling
Shipping AMBIENT
Short Term Storage +20°C
Long Term Storage +4°C
Handling Advice Keep cool and dry.
Use/Stability Stable for at least 2 years after receipt when stored at +4°C.
Documents
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
Description
  • Mitochondrial pyruvate dehydrogenase kinase (PDK) inhibitor, consequently activating pyruvate dehydrogenase (PDH). 
  • Decreases glycolysis. Shifts pyruvate metabolism from glycolysis and lactate production to glucose oxidation in the mitochondria. 
  • Antitumor agent. Decreases tumor growth in vitro and in vivo. Induces mitochondrial-dependent apoptosis.
  • Useful agent for immunometabolism research.
  • Glucose entering the cell is metabolized by glycolysis to pyruvate. Most of the pyruvate in non-cancerous cells enters the mitochondria under aerobic conditions and a small fraction is metabolized to lactate. PDH in mitochondria converts pyruvate into acetyl-CoA, which enters the TCA cycle. In cancer cells, the oxidative (mitochondrial) pathway of glucose utilization is suppressed and most of the pyruvate is converted into lactate (Warburg effect). The relative activities of LDH and PDH therefore determine the fate of pyruvate. PDK inhibits PDH through phosphorylation and regulates its activities, resulting in suppression of the TCA cycle and mitochondrial respiration. This renders PDK a promising target for the treatment of various cancers.
Product References
  1. Activation of pyruvate dehydrogenase in perfused rat heart by dichloroacetate: S. Whitehouse & P.J. Randle; Biochem. J. 134, 651 (1973)
  2. The pharmacology of dichloroacetate: P.W. Stacpoole; Metabolism 38, 1124 (1989)
  3. A mitochondria-K+ channel axis is suppressed in cancer and its normalization promotes apoptosis and inhibits cancer growth: S. Bonnet, et al.; Cancer Cell 11, 37 (2007)
  4. Distinct Structural Mechanisms for Inhibition of Pyruvate Dehydrogenase Kinase Isoforms by AZD7545, Dichloroacetate, and Radicicol: M. Kato, et al.; Cell Structure 15, 992 (2007)
  5. Metabolic Modulation of Glioblastoma with Dichloroacetate: E.D. Michelakis, et al.; Sci. Transl. Med. 2, 31 (2010)
  6. PDK1 inhibition is a novel therapeutic target in multiple myeloma: S. Fujiwara, et al.; Br. J. Cancer 108, 170 (2013)1
  7. A guide to immunometabolism for immunologists: L.A. O'Neill, et al.; Nat. Rev. Immunol. 16, 553 (2016)
  8. The pyruvate dehydrogenase complex in cancer: An old metabolic gatekeeper regulated by new pathways and pharmacological agents: E. Saunier, et al.; Int. J. Cancer 138, 809 (2016) (Review) 
  9. The PDK1 Inhibitor Dichloroacetate Controls Cholesterol Homeostasis Through the ERK5/MEF2 Pathway: A.U. Haq Khan, et al.; Nat. Sci. Rep. 7, 10654 (2017)
  10. Dichloroacetate induces regulatory T-cell differentiation and suppresses Th17-cell differentiation by pyruvate dehydrogenase kinase-independent mechanism: N. Makita, et al.; J. Pharm. Pharmacol. 69, 43 (2017)
© 2017 Adipogen Life Sciences. Pictures: © 2012 Martin Oeggerli. All Rights Reserved.