Home Metabolism Dehydrogenase inhibitor - AhR agonist Leflunomide For research use only.

Leflunomide

Synonyms: HWA486, RS-34821, SU101

Leflunomide is a pyrimidine synthesis and protein tyrosine kinase inhibitor belonging to the DMARD, used as an immunosuppressant agent. The active metabolite of Leflunomide is A77 1726, which inhibits dihydroorotate dehydrogenase (DHODH). Leflunomide is also an agonist of the AhR.

Leflunomide Chemical Structure

Leflunomide Chemical Structure

CAS No. 75706-12-6

Purity & Quality Control

Leflunomide Related Products

Signaling Pathway

Dehydrogenase Signaling Pathways

Dehydrogenase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
B-cells Function assay In vitro inhibition of Ab formation from trinitrophenyl-lipopolysaccharide (TNP-LPS) B-cells, IC50=5.1μM 11384243
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
Click to View More Cell Line Experimental Data

Biological Activity

Description Leflunomide is a pyrimidine synthesis and protein tyrosine kinase inhibitor belonging to the DMARD, used as an immunosuppressant agent. The active metabolite of Leflunomide is A77 1726, which inhibits dihydroorotate dehydrogenase (DHODH). Leflunomide is also an agonist of the AhR.
Targets
Dihydroorotate dehydrogenase [1]
In vitro
In vitro Leflunomide is actually a prodrug that is processed in vivo to the active metabolite A771726，which has been shown to inhibit proliferation of mononuclear and T-cells. Leflunomide is an inhibitor of several protein tyrosine kinases, with IC50 values between 30 mM and 100 mM in vitro cellular and enzymatic assays. [1] Leflunomide is capable of inhibiting anti-CD3- and interleukin-2 (IL-2)-stimulated T cell proliferation. Leflunomide is able to inhibit p59fyn and p56lck activity in in vitro tyrosine kinase assays. Leflunomide also inhibits Ca2+ mobilization in Jurkat cells stimulated by anti-CD3 antibody but not in those stimulated by ionomycin. Leflunomide also inhibits distal events of anti-CD3 monoclonal antibody stimulation, namely, IL-2 production and IL-2 receptor expression on human T lymphocytes. Leflunomide also inhibits tyrosine phosphorylation in CTLL-4 cells stimulated by IL-2. [2] Leflunomide is an immunomodulatory drug that may exert its effects by inhibiting the mitochondrial enzyme dihydroorotate dehydrogenase (DHODH), which plays a key role in the de novo synthesis of the pyrimidine ribonucleotide uridine monophosphate (rUMP). Leflunomide prevents the expansion of activated and autoimmune lymphocytes by interfering with the cell cycle progression due to inadequate production of rUMP and utilizing mechanisms involving p53. [3]
Experimental Result Images Methods Biomarkers Images PMID
Growth inhibition assay Cell viability 29423085
Western blot DH0DH ATF4 / CHOP CDK2 / Cyclin A2 23977077
In Vivo
In vivo Leflunomide is able to prevent and reverse allograft and xenograft rejection in rodents, dogs, and monkeys. [2]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05605587 Recruiting
MEN1 Gene Mutation
University Hospital Basel Switzerland
 May 2 2023 Not Applicable
NCT04212416 Active not recruiting
Chronic Graft Versus Host Disease|Steroid Refractory Graft Versus Host Disease
City of Hope Medical Center|National Cancer Institute (NCI)
 May 12 2020 Phase 1
NCT04361214 Terminated
COVID-19
University of Chicago
 May 5 2020 Phase 1
NCT03715699 Unknown status
Autoimmune Disease
Peking Union Medical College Hospital
 July 1 2018 Not Applicable
NCT03599986 Completed
Active Rheumatoid Arthritis
Eva Pharma|DataClin
 June 16 2017 --

Chemical Information & Solubility

Molecular Weight 270.21 Formula

C12H9F3N2O2
CAS No. 75706-12-6 SDF Download Leflunomide SDF
Smiles CC1=C(C=NO1)C(=O)NC2=CC=C(C=C2)C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 54 mg/mL ( (199.84 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 54 mg/mL

Water : 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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