Brequinar sodium
Dihysroorotate dehydrogenase inhibitor, antiviral / Brequinar sodium is an inhibitor of dihydroorotate dehydrogenase (DHODH)1,2 with IC50’s between 0.2 and 5.8 µM in various cell lines3 and 20 nM in isolated enzyme4. It reduced leukemic cell burden, decreased levels of leukemia-initiating cells, and improved survival in human and mouse models of acute myeloid leukemia.4 Brequinar displayed broad antiviral activity against flaviviruses, positive-strand RNA alphaviruses, negative-strand RNA rhabdoviruses, Influenza A and B viruses, and HIV.5,6,7
Biochemicals & reagents
96201-88-6
DuP-785; NSC 368390
1) Chen et al. (1986) Mechanism of action of the novel anticancer agent 6-fluoro-2-(2'-fluoro-1,1'-biohenyl-4-yl)-3-methyl-4-quinolinecarboxylic acid sodium salt (NSC 368390): inhibition of de novo pyrimidine nucleotide biosynthesis, Cancer Res. 46 5014 2) Peters et al. (1990) In vivo inhibition of the pyrimidine de novo enzyme dihydroorotic aicd dehydrogenase by brequinar sodium (DUP-785; NSC 368390) in mice and patients, Cancer Res. 50 4644 3) De Kant et al. (1989) The relation between inhibition of cell growth and of duhydroorotic acid dehydrogenase by brequinar sodium, Cancer Lett. 46 123 4) Sykes et al. (2016) Inhibition of Dihydroorotate Overcomes Differentiation Blockade in Acute Myeloid Leukemia, Cell 167 171 5) Qing et al. (2010) Characterization of Dengue Virus Resistance to Brequinar in Cell Culture, Antimicrob. Agents Chemother. 54 3686 6) Andersen et al. (2019) Novel Antiviral Activities of Obatoclax, Emetine, Niclosamide, Brequinar, and Homoharringtonine, Viruses 11 E964 7) Park et al. (2020) Identification and Characterization of Novel Compounds with Broad-Spectrum Antiviral Activity against Influenza A and B Viruses, J. Virol. 94 e02149
-20°C
TARGET: Dehydrogenase (GAPDH, GPDH, IMPDH, PHGDH, LDH, DHODH, ALDH, GDH, IDH, UGDH, DPD, DHPDH, KGDH, PDH, and MDH) -- PATHWAY: Nucleoside/tide biosynthesis; DNA synthesis; Ferroptosis; Mitochondrial function -- RESEARCH AREA: Immunology; Cell death -- DISEASE AREA: Cancer; Infectious diseaseInflammation