Brequinar

Brequinar (DUP785) is a potent inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of 5.2 nM for human DHODH. Brequinar has potent activities against a broad spectrum of viruses. Brequinar also has an anti-SARS2 activity.

Product Specifications

CAS Number

[96187-53-0]

Product Name Alternative

DUP785; NSC 368390

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Dihydroorotate Dehydrogenase; DNA/RNA Synthesis; SARS-CoV; Virus Protease

Type

Reference compound

Related Pathways

Anti-infection; Cell Cycle/DNA Damage; Metabolic Enzyme/Protease

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Infection; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/Brequinar.html

Purity

99.89

Solubility

DMSO : 25 mg/mL (ultrasonic) |Ethanol : < 1 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(C1=C(C)C(C2=CC=C(C3=CC=CC=C3F)C=C2)=NC4=CC=C(F)C=C14)O

Molecular Formula

C23H15F2NO2

Molecular Weight

375.37

Precautions

H302, H315, H319, H335

References & Citations

[1]Schnellrath LC, et al. Potent antiviral activity of brequinar against the emerging Cantagalo virus in cell culture. Int J Antimicrob Agents. 2011 Nov;38 (5) :435-41.|[2]Qing M, et al. Characterization of dengue virus resistance to brequinar in cell culture. Antimicrob Agents Chemother. 2010 Sep;54 (9) :3686-95.|[3]Xu X, et al. In vitro and in vivo mechanisms of action of the antiproliferative and immunosuppressive agent, brequinar sodium. J Immunol. 1998 Jan 15;160 (2) :846-53.|[4]Zeping Zuo, et al. Bifunctional Naphtho[2,3-d][1,2,3]triazole-4,9-dione Compounds Exhibit Antitumor Effects In Vitro and In Vivo by Inhibiting Dihydroorotate Dehydrogenase and Inducing Reactive Oxygen Species Production. J Med Chem. 2020 Jun 4.|[5]David C Schultz, et al. Pyrimidine inhibitors synergize with nucleoside analogues to block SARS-CoV-2. Nature. 2022 Feb 7.