Brequinar (Synonyms: DUP785; NSC 368390)

Cat. No.: HY-108325 Purity: 99.75%: FAQs
Data Sheet SDS COA Handling Instructions

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.

For research use only. We do not sell to patients.

Brequinar Chemical Structure

CAS No. : 96187-53-0

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10 mM * 1 mL in DMSO	USD 92	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 7 publication(s) in Google Scholar

7 Publications Citing Use of MCE Brequinar

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Description

In Vitro

Brequinar reduces virus progeny production by >90%, with EC₅₀ of 17 nM. Brequinar (5 μM) also inhibits other orthopoxviruses, and blocks virus DNA replication. Brequinar does not affect virus early gene expression, but has a severe effect on the late stage of the virus cycle^[1]. Brequinar reduces the level of envelope protein production and the viral titer in a dose-dependent manner, with EC₅₀ of 78 nM in the CFI assay. Brequinar (5 μM) inhibits viral RNA synthesis. Brequinar has antiviral effect, but the effect is reversed by pyrimidine. Brequinar-resistant viruses can be selected in cell culture. Brequinar (5 μM) suppresses the luciferase activities from both the WT and NS5 mutant replicons^[2]. Brequinar sodium effectively prevents the increase in PyNTP levels with an IC₅₀ of 0.26 μM. Brequinar sodium effectively inhibits cell proliferation with an IC₅₀ of 0.26 μM. Brequinar sodium inhibits autophosphorylation of p56^lck with IC₅₀ of 70 μM; inhibition is 39, 41, and 60% for 25, 50, and 100 μM Brequinar sodium, respectively. Brequinar sodium also inhibits the phosphorylation by p56^lck of the exogenous substrate, histone 2B, with an IC₅₀ of 70 μM; inhibition is 10, 43, 59, and 86% for 25, 50, 100, and 200 μM Brequinar sodium, respectively. Brequinar sodium inhibits autophosphorylation of p59^fyn with an IC₅₀ of 105 μM; inhibition is 0, 17, 48, and 65% for 25, 50, 100, and 200 μM Brequinar sodium, respectively. Brequinar sodium also inhibits the phosphorylation by p59^fyn of histone 2B with an IC₅₀ of 20 μM; inhibition is 26, 54, 79, 83, and 84% for 10, 25, 50, 100, and 200 μM Brequinar sodium, respectively^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Brequinar sodium-treated (10-20 mg/kg/day) mice has a 31% reduction in percentage of packed cell volume compared with untreated BALB/c mice. Brequinar sodium reduces UTP and CTP levels in bone marrow cells by 30 and 25%, respectively. Brequinar sodium (10-20 mg/kg/day) in combination with uridine (1000-2000 mg/kg/day) prevents anemia, and the hematocrits remain at levels (61-63%) comparable with those of untreated controls^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

375.37

Appearance

Solid

Formula

C₂₃H₁₅F₂NO₂

CAS No.

96187-53-0

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (66.60 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6640 mL	13.3202 mL	26.6404 mL
5 mM	0.5328 mL	2.6640 mL	5.3281 mL
10 mM	0.2664 mL	1.3320 mL	2.6640 mL

*Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.08 mg/mL (5.54 mM); Suspended solution; Need ultrasonic and warming
2.

Add each solvent one by one: 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.54 mM); Clear solution

*All of the co-solvents are available by MCE.

Purity & Documentation

Purity: 99.75%

Select Batch:

Data Sheet (282 KB) SDS (392 KB)

COA (250 KB) HNMR (283 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[2]. Qing M, et al. Characterization of dengue virus resistance to brequinar in cell culture. Antimicrob Agents Chemother. 2010 Sep;54(9):3686-95. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[5]. David C Schultz, et al. Pyrimidine inhibitors synergize with nucleoside analogues to block SARS-CoV-2. Nature. 2022 Feb 7. [Content Brief]

Kinase Assay ^[3]	Immunoprecipitated p59^fyn or p56^lck from CTLL-4 cells or LSTRA cells (5×10⁶) is preincubated with various concentrations of BQR in the PTK buffer (50 mM HEPES (pH 7.4), 10 mM MgCl₂, and 10 mM MnCl₂) on ice for 10 min. Exogenous substrate, histone 2B (2 μg), is added and, after 10 min, the reaction is initiated by addition of 10 μCi [γ-³²P]ATP. After incubation at 20°C for 10 min, the reaction mixture is subjected to electrophoresis in a 12.5% SDS-polyacrylamide gel. Phosphorylation of the kinase and the exogenous substrate is analyzed by autoradiography. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	The neutral-red uptake assay is used to evaluate cell viability. BSC-40 cells are seeded in 96-well plates in the presence of concentrations of Brequinar ranging from 0.01 μM to 75 μM for 24 h. Control cells are incubated with 0.1% DMSO. Neutral red is methanol/acetic acid-extracted from cells and is quantitated at an absorbance of 490 nm (A490). All measurements expressed the average of four independent assays. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Brequinar is administered once daily by i.p. injection, while uridine is administered twice daily. Mice are bled through the orbital vein using a microhematocrit capillary tube, and the blood is centrifuged for 10 min at 550 × g. The percentage of packed cell volumes is determined with a microhematocrit capillary tube reader. All mice are killed 4 h after receiving their last dose of Brequinar or uridine. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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. [Content Brief] [2]. Qing M, et al. Characterization of dengue virus resistance to brequinar in cell culture. Antimicrob Agents Chemother. 2010 Sep;54(9):3686-95. [Content Brief] [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. [Content Brief] [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. [Content Brief] [5]. David C Schultz, et al. Pyrimidine inhibitors synergize with nucleoside analogues to block SARS-CoV-2. Nature. 2022 Feb 7. [Content Brief]

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Brequinar96187-53-0DUP785 NSC 368390DUP 785DUP-785NSC368390NSC 368390NSC-368390Dihydroorotate DehydrogenaseSARS-CoVVirus ProteaseDNA/RNA SynthesisDHODHSARS coronavirusInhibitorinhibitorinhibit

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Brequinar (Synonyms: DUP785; NSC 368390)

Customer Review

7 Publications Citing Use of MCE Brequinar

Featured Recommendations

•Related Screening Libraries:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

Your Recently Viewed Products:

Customer Review

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