Home Metabolism Dehydrogenase inhibitor Brequinar For research use only.

Brequinar

Synonyms: DUP785, NSC 368390

Brequinar is an inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of ∼20 nM in vitro.

Brequinar Chemical Structure

Brequinar Chemical Structure

CAS No. 96187-53-0

Purity & Quality Control

Brequinar Related Products

Signaling Pathway

Dehydrogenase Signaling Pathways

Dehydrogenase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
insect cells Function assay Inhibition of human recombinant DHODH expressed in baculovirus infected insect cells using dihydroorotate as substrate in presence of quinone by dichlorophenol-indophenol dye based assay, IC50=0.01μM 27994748
A549 Antiviral assay Antiviral activity against Yellow fever virus infected in human A549 cells assessed as reduction in virus replication, EC50=0.078μM 31557612
A549 Antiviral assay Antiviral activity against West Nile virus infected in human A549 cells assessed as reduction in virus replication, EC50=0.078μM 31557612
A549 Antiviral assay Antiviral activity against Dengue virus infected in human A549 cells assessed as reduction in virus replication, EC50=0.078μM 31557612
A549 Antiviral assay Antiviral activity against Western equine encephalomyelitis virus infected in human A549 cells assessed as reduction in virus replication, EC50=0.078μM 31557612
A549 Antiviral assay Antiviral activity against Vesicular stomatitis virus infected in human A549 cells assessed as reduction in virus replication, EC50=0.078μM 31557612
Jurkat Antiproliferative assay 72 hrs Inhibition of cell proliferation of human Jurkat cells incubated for 72 hrs by Celltiter-Glo assay, IC50=0.2μM 26079043
MDCK Antiviral assay 48 hrs Antiviral activity against VSV infected in MDCK cells assessed as inhibition of VSV replication after 48 hrs by plaque assay, EC50=0.3μM 23930152
MDCK Antiviral assay 48 hrs Antiviral activity against influenza A virus A/WSN/33 (H0N1) infected in MDCK cells after 48 hrs by plaque assay, EC50=0.46μM 23930152
HL60 Antiproliferative assay 72 hrs Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay, IC50=0.544μM 29727569
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells over-expressing DHODH after 72 hrs by MTT assay, IC50=0.679μM 29727569
Jurkat T Antiproliferative assay 72 hrs Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye-based fluorescence assay, IC50=0.91μM 29939742
Jurkat T Antiproliferative assay 72 hrs Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye based fluorometric method, IC50=0.93μM 28235702
MIAPaCa2 Antiproliferative assay 72 hrs Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by MTT assay, IC50=1.69μM 29727569
Jurkat T Cytotoxicity assay 72 hrs Cytotoxicity against human Jurkat T cells assessed as compound concentration required to induce up to 30% cell death after 72 hrs by Hoechst 33258 dye based fluorometric method, Activity=45μM 28235702
Jurkat T Cytotoxicity assay 72 hrs Cytotoxicity against human Jurkat T cells assessed as compound concentration required to induce =>30% cell death after 72 hrs by CellTox green assay, Activity=48.2μM 29939742
HCT116 Growth inhibition assay 72 hrs Growth inhibition of human HCT116 cells over-expressing DHODH at 2 times antiproliferative IC50 after 72 hrs in absence of uridine by MTT assay 29727569
HCT116 Cytostatic activity assay 10 uM 24 hrs Cytostatic activity against human HCT116 cells assessed as reduction in colony forming at 10 uM after 24 hrs by crystal violet staining based assay 29727569
HCT116 Cytostatic activity assay 10 uM 7 days Cytostatic activity against human HCT116 cells assessed as reduction in colony forming at 10 uM after 7 days by crystal violet staining based assay 29727569
U937 Antiproliferative assay 0.01 to 10 uM 3 days Antiproliferative activity against CFSE-labeled human U937 cells at 0.01 to 10 uM after 3 days by propidium iodide staining-based flow cytometry 29939742
THP1 Antiproliferative assay 0.01 to 10 uM 3 days Antiproliferative activity against CFSE-labeled human THP1 cells at 0.01 to 10 uM after 3 days by propidium iodide staining-based flow cytometry 29939742
U937 Function assay 0.1 to 10 uM up to 4 days Induction of myeloid differentiation in human U937 cells assessed as increase in CD11b expression level at 0.1 to 10 uM up to 4 days by propidium iodide staining-based flow cytometry 29939742
THP1 Function assay 0.1 to 10 uM up to 5 days Induction of myeloid differentiation in human THP1 cells assessed as increase in CD11b expression level at 0.1 to 10 uM up to 5 days by propidium iodide staining-based flow cytometry 29939742
THP1 Function assay 0.1 to 10 uM up to 5 days Induction of myeloid differentiation in human THP1 cells assessed as increase in CD14 expression level at 0.1 to 10 uM up to 5 days by propidium iodide staining-based flow cytometry 29939742
Click to View More Cell Line Experimental Data

Biological Activity

Description Brequinar is an inhibitor of dihydroorotate dehydrogenase (DHODH) with an IC50 of ∼20 nM in vitro.
Targets
DHODH [1]
20 nM
In vitro
In vitro

Brequinar sodium (BQR) reduces of PyN levels in Con A-stimulated T cells and inhibition of cell proliferation at low concentrations, which can be reversed by uridine. However, uridine is unable to reverse the effects of high concentrations of BQR. BQR possesses the ability of inhibiting tyrosine phosphorylation.[2]
Cell Research Cell lines splenic T cells isolated from BALB/c mice
Concentrations 0.26, 1.3, 2.6 μM
Incubation Time 40-66 h
Method

Lymphocytes are isolated from BALB/c spleen by centrifugation through a Ficol gradient and are depleted of macrophages and B cells by adherence to goat anti-mouse IgG-coated plates. The nonadherent cells are harvested and cultured at 4 to 5× 105/ml in RPMI 1640 supplemented with 10% FBS. Stimulation is performed with 5 μg/ml Con A in the presence of indicated concentrations of Brequinar or uridine. After 40 to 66 h, the cells are harvested and the levels of cell proliferation or purine NTP and PyNTP are quantified.
In Vivo
In vivo

Brequinar sodium (BQR) induces anemia through inhibition of DHO-DHase activity and de novo pyrimidine synthesis in vivo. Coadministration of BQR with uridine prevents anemia.[2]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03760666 Terminated
Acute Myeloid Leukemia
Clear Creek Bio Inc.
 December 20 2018 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 375.37 Formula

C23H15F2NO2
CAS No. 96187-53-0 SDF --
Smiles CC1=C(C2=C(C=CC(=C2)F)N=C1C3=CC=C(C=C3)C4=CC=CC=C4F)C(=O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 37 mg/mL ( (98.56 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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