Brequinar

• CAT Number: I000013
• CAS Number: 96187-53-0
• Molecular Formula: C23H15F2NO2
• Molecular Weight: 375.37
• Purity: ≥95%
• Target: DODH inhibitor
• Storage: Store at -20°C

Brequinar (CAT: I000013) is a potent and selective inhibitor of dihydroorotate dehydrogenase (DHODH), an enzyme involved in de novo pyrimidine synthesis. By blocking DHODH, brequinar interferes with the production of DNA and RNA, inhibiting the proliferation of rapidly dividing cells. Brequinar has shown antitumor activity and has been investigated for its potential use in cancer treatment. Additionally, it has been studied in the context of autoimmune diseases and viral infections. Further research is ongoing to explore its therapeutic applications and optimize its efficacy and safety profile.

Reference

1:Inhibition of the mitochondrial pyrimidine biosynthesis enzyme dihydroorotate dehydrogenase by doxorubicin and brequinar sensitizes cancer cells to TRAIL-induced apoptosis. He T, Haapa-Paananen S, Kaminskyy VO, Kohonen P, Fey V, Zhivotovsky B, Kallioniemi O, Perälä M.Oncogene. 2014 Jul 3;33(27):3538-49. doi: 10.1038/onc.2013.313. Epub 2013 Sep 9. PMID: 24013224 2:Potent antiviral activity of brequinar against the emerging Cantagalo virus in cell culture. Schnellrath LC, Damaso CR.Int J Antimicrob Agents. 2011 Nov;38(5):435-41. doi: 10.1016/j.ijantimicag.2011.07.002. Epub 2011 Aug 12. PMID: 21840180 Free Article3:Characterization of dengue virus resistance to brequinar in cell culture. Qing M, Zou G, Wang QY, Xu HY, Dong H, Yuan Z, Shi PY.Antimicrob Agents Chemother. 2010 Sep;54(9):3686-95. doi: 10.1128/AAC.00561-10. Epub 2010 Jul 6. PMID: 20606073 Free PMC Article4:Brequinar derivatives and species-specific drug design for dihydroorotate dehydrogenase. Hurt DE, Sutton AE, Clardy J.Bioorg Med Chem Lett. 2006 Mar 15;16(6):1610-5. Epub 2006 Jan 10. PMID: 16406782 5:Synthesis of brequinar analogue inhibitors of malaria parasite dihydroorotate dehydrogenase. Boa AN, Canavan SP, Hirst PR, Ramsey C, Stead AM, McConkey GA.Bioorg Med Chem. 2005 Mar 15;13(6):1945-67. PMID: 15727850 6:Multiple inhibitor analysis of the brequinar and leflunomide binding sites on human dihydroorotate dehydrogenase. McLean JE, Neidhardt EA, Grossman TH, Hedstrom L.Biochemistry. 2001 Feb 20;40(7):2194-200. PMID: 11329288 7:Brequinar in combination with cyclosporine a inhibits islet xenograft rejection for up to 24 days: a study in the pig-to-rat model. Wennberg L, Song Z, Wijkström M, Zhang J, Bari S, Sundberg B, Groth CG, Korsgren O.Transplant Proc. 2000 Aug;32(5):1026. No abstract available. PMID: 10936333 8:Kinetics of inhibition of human and rat dihydroorotate dehydrogenase by atovaquone, lawsone derivatives, brequinar sodium and polyporic acid. Knecht W, Henseling J, Löffler M.Chem Biol Interact. 2000 Jan 3;124(1):61-76. PMID: 10658902 9:Immunosuppressive effect of combination schedules of brequinar with leflunomide or tacrolimus on rat cardiac allotransplantation. Antoniou EA, Deroover A, Howie AJ, Chondros K, McMaster P, D/’Silva M.Microsurgery. 1999;19(2):98-102. PMID: 10188834 10:Heteroatom- and carbon-linked biphenyl analogs of Brequinar as immunosuppressive agents. Batt DG, Petraitis JJ, Sherk SR, Copeland RA, Dowling RL, Taylor TL, Jones EA, Magolda RL, Jaffee BD.Bioorg Med Chem Lett. 1998 Jul 7;8(13):1745-50. PMID: 9873427