Leflunomide (HWA486)

For research use only.

Catalog No.S1247 Synonyms: RS-34821, SU101, Arava

9 publications

Leflunomide (HWA486) Chemical Structure

CAS No. 75706-12-6

Leflunomide (HWA486, RS-34821, SU101, Arava) 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.

Selleck's Leflunomide (HWA486) has been cited by 9 publications

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  • Peritoneal macrophages were pretreated for 1 h with the leflunomide (100 umol/L), followed by treatment with 10 ug/ml rTsP53 for 6 h. Western blot analysis of P-STAT6 and STAT6 expression was performed. Corresponding staining for b-actin was carried out to control for equal loading. *P < 0.05 versus control group, #P < 0.05 versus rTsP53 group.

    Cell Immunol 2014 288(1-2), 1-7. Leflunomide (HWA486) purchased from Selleck.

    Peritoneal macrophages were stained for FITC-MR. Flow cytometry analysis of MFI. The result for one representative of three independent experiments is shown.

    Cell Immunol 2014 288(1-2), 1-7. Leflunomide (HWA486) purchased from Selleck.

  • We found that the expression of Arg1, Ym1 and IL-10 on peritoneal macrophages incubated with leflunomide and rTsP53 were significantly down-regulated in comparison to treatment with rTsP53 alone.

    Cell Immunol 2014 288(1-2), 1-7. Leflunomide (HWA486) purchased from Selleck.

    H1299, H460, A549 cells were treated with leflunomide or teriflunomide at indicated concentrations for 24 h.

    Toxicol Lett, 2018, . Leflunomide (HWA486) purchased from Selleck.

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Biological Activity

Description Leflunomide (HWA486, RS-34821, SU101, Arava) 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.
Dihydroorotate dehydrogenase [1]
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
B-cells MkfWSpVv[3Srb36gZZN{[Xl? M4XVfGlvKH[rdILvJIlvcGmkaYTpc44hd2ZiQXKg[o9zdWG2aX;uJIZzd21idILpcol1em:yaHXufYwudGmyb4DvcJl{[WOlaHHybYRmKCiWTmCtUHBUMSCELXPlcIx{NCCLQ{WwQVUvOc7:TR?= NVTvb4d7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUGzPFQzPDNpPkGxN|g1OjR|PD;hQi=>
A673 NH;xOItyUFSVIHHzd4F6 NGO0PGlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?= M{j6dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC NYTufHREeUiWUzDhd5NigQ>? MV3xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC MljSdWhVWyCjc4PhfS=> M1;yS5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vTVOgZ4VtdHN? NV7sPVZTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>

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Methods Test Index PMID
Growth inhibition assay
Cell viability; 

PubMed: 29423085     

Leflunomide causes a dose-dependent decrease in cell viability in eight human melanoma cell lines. BRAFWT cell lines; M202 (blue), M285 (red), M375 (green) and M296 (purple). BRAFV600E mutant cell lines; A375 (orange), M229 (grey), SKmel28 (khaki) and SKmel5 (black). Cell viability was determined by using CellTiter-Glo reagent and all values are represented as a percentage (%) relative to the vehicle control. Data is presented as the mean ± SEM of three independent experiments each performed with cell culture triplicates. 

Western blot

PubMed: 23977077     

The DHODH protein expression levels were detected by western blotting in three neuroblastoma cell lines treated with either DMSO or 100 µM leflunomide for 72 hours. α-tubulin as the control.

ATF4 / CHOP ; 

PubMed: 29427785     

Glucose-grown and galactose-grown HepG2 cells were exposed to 50 to 300 μM of leflunomide for 6 h. Western blot showed that galactose-grown HepG2 cells exhibited more prominent increase in both ATF4 and CHOP protein levels. 

CDK2 / Cyclin A2 ; 

PubMed: 29348830     

Western blot assay was performed to assess the cell cycle-related protein levels in A375 and MV3 cells after treatment with leflunomide for 0, 24, 48, 72 and 96 hours. Tubulin was used as a loading control.

23977077 29427785 29348830
In vivo Leflunomide is able to prevent and reverse allograft and xenograft rejection in rodents, dogs, and monkeys. [2]


Solubility (25°C)

In vitro DMSO 54 mg/mL (199.84 mM)
Water Insoluble
Ethanol ''54 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 270.21


CAS No. 75706-12-6
Storage powder
in solvent
Synonyms RS-34821, SU101, Arava
Smiles CC1=C(C=NO1)C(=O)NC2=CC=C(C=C2)C(F)(F)F

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04212416 Recruiting Drug: Leflunomide 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 Recruiting Drug: Leflunomide COVID-19 University of Chicago May 5 2020 Phase 1
NCT03715699 Unknown status Drug: Prednisone|Drug: Prednisone and Leflunomide Autoimmune Disease Peking Union Medical College Hospital July 1 2018 Not Applicable
NCT03599986 Completed -- Active Rheumatoid Arthritis Eva Pharma|DataClin June 16 2017 --
NCT01500551 Recruiting Drug: Tofacitinib Juvenile Idiopathic Arthritis Pfizer March 18 2013 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID