A quinolinecarboxylic acid derivative with immunosuppressive and anti-neoplastic properties. Inhibits pyrimidine synthesis by blocking the activity of mammalian mitochondrial dihydroorotate dehydrogenase (DHODH; IC50 = 12 nM). Does not affect DHODH in non-mammalian species. Also reported to inhibit glycosylation of adhesion molecules. Potentiates the sensitivity of U1690 small cell lung cancer cells to TRAIL-induced apoptosis and synergistically enhances the anti-tumor effects of doxorubicin ( ~100 µM).
Biochem/physiol Actions
Cell permeable: yes
Primary Target DHODH
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
He, T. et al. 2013. Oncogene32, in press. Hurt, D.E., et al. 2006. Bioorg. Med. Chem. Lett.16, 1610. Schnellrath, L. et al. 2011. Int. J. Antimicrob. Agents.38, 435. Batt, D.G., et al. 1995. Bioorg. Med. Chem. Lett.14, 1549. Allison, A., et al. 1993. Transplantation Proc.25, 67. Cramer, D. et al. 1992. Transplantation.53, 303.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
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