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Chemical Compound Review:

CHEMBL82479 2,3,5-trimethyl-6-(pyridin- 3...

Synonyms: AG-D-39515, SureCN2715544, ACMC-20mn9v, CV-6504, CHEBI:228590, ...

Hussey, H.J. et al., Hussey, H.J. et al., Whitehouse, A.S. et al., Ohkawa, S. et al., Hussey, H.J. et al.

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Disease relevance of CV-6504

2,3,5-Trimethyl-6-(3-pyridylmethyl)1,4-benzoquinone (CV-6504) is an effective inhibitor of the growth of established murine adenocarcinomas (MACs) and is shortly to enter clinical investigation [1].

High impact information on CV-6504

Two other cell lines, MDA-MB-231 and PC-3, sensitive to growth inhibition by CV-6504, are known to require LA for growth, while DU-145, which was insensitive to growth inhibition by CV-6504, showed no growth response to LA [2].
Novel anti-tumour activity of 2,3,5-trimethyl-6-(3-pyridylmethyl)-1,4- benzoquinone (CV-6504) against established murine adenocarcinomas (MAC) [3].
2,3,5-Trimethyl-6-(3-pyridylmethyl)1,4-benzoquinone (CV-6504), an inhibitor of 5-lipoxygenase and thromboxane A2 synthase and a scavenger of active oxygen species, has been shown to exhibit profound anti-tumour activity against three established murine adenocarcinomas (MACs) that are generally refractory to standard cytotoxic agents [3].
Metabolism and pharmacokinetics of the anti-tumour agent 2,3,5-trimethyl-6-(3-pyridylmethyl)1,4-benzoquinone (CV-6504) [1].
After 24 h, the concentration of free CV-6504 in the tumour (3.3 microM) was higher than that in the liver (0.24 microM) and equal to the IC50 value for the inhibition of the growth of MAC16 cells in vitro (3 microM) [1].

Biological context of CV-6504

Therefore, it can be concluded that CV-6504 is reduced mainly by two electron donating enzymes without the intermediary of a semiquinone radical and that the resulting hydroquinone inhibits lipid peroxidation as well as 5-lipoxygenase activity [4].

Associations of CV-6504 with other chemical compounds

Tumour sensitivity may be correlated with increased DT-diaphorase that are required to metabolise CV-6504 to the active hydroquinone, which inhibits 5-lipoxygenase activity [3].

Gene context of CV-6504

However, 2,3,5-trimethyl-6-(3-pyridylmethyl)1,4-benzoquinone (CV-6504), an inhibitor of 5-, 12- and 15-lipoxygenases also attenuated muscle protein catabolism, proteasome "chymotryptic-like" enzyme activity and expression of proteasome 20S alpha-subunits in soleus muscles from acute fasted mice [5].

References

Metabolism and pharmacokinetics of the anti-tumour agent 2,3,5-trimethyl-6-(3-pyridylmethyl)1,4-benzoquinone (CV-6504). Hussey, H.J., Tisdale, M.J. Br. J. Cancer (1996) [Pubmed]
Mechanism of the anti-tumour effect of 2,3,5-trimethyl-6-(3-pyridylmethyl) 1,4-benzoquinone (CV-6504). Hussey, H.J., Tisdale, M.J. Br. J. Cancer (1997) [Pubmed]
Novel anti-tumour activity of 2,3,5-trimethyl-6-(3-pyridylmethyl)-1,4- benzoquinone (CV-6504) against established murine adenocarcinomas (MAC). Hussey, H.J., Bibby, M.C., Tisdale, M.J. Br. J. Cancer (1996) [Pubmed]
Reduction of 2,3,5-trimethyl-6-(3-pyridylmethyl)-1,4-benzoquinone by PB-3c cells and biological activity of its hydroquinone. Ohkawa, S., Terao, T., Murakami, M., Matsumoto, T., Goto, G. Chem. Pharm. Bull. (1991) [Pubmed]
Downregulation of ubiquitin-dependent proteolysis by eicosapentaenoic acid in acute starvation. Whitehouse, A.S., Tisdale, M.J. Biochem. Biophys. Res. Commun. (2001) [Pubmed]

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