Leflunomide [75706-12-6]

Cat# HY-B0083-100mg

Size : 100mg

Brand : MedChemExpress

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Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase (DHODH), and acts as a disease-modifying antirheumatic agent.

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

Leflunomide Chemical Structure

CAS No. : 75706-12-6

*

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WB
    Western blot analysis the changes of apoptosis-associated protein at day 18 of HL60 xenograft tumors treated with vehicle, Isobavachalcone (IBC) or Leflunomide (LEF). Expression levels of MYC and p21 in vehicle, IBC, or LEF treated tumors are estimated by western blot.
    Western blot indicates that the expression of pSTAT6 and CCL26 in HCC cells induced by ectopic NDRG1 expression is obviously attenuated by LEF treatment.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase (DHODH), and acts as a disease-modifying antirheumatic agent.

    In Vitro

    Leflunomide is actually a prodrug that 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.
    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.
    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.

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

    • [1]. Davis JP, et al. The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase. Biochemistry. 1996 Jan 30;35(4):1270-3.  [Content Brief]

      [2]. Xu X, et al. Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide. J Biol Chem. 1995 May 26;270(21):12398-403.  [Content Brief]

      [3]. Fox RI, et al. Mechanism of action for leflunomide in rheumatoid arthritis. Clin Immunol. 1999 Dec;93(3):198-208.  [Content Brief]

    DHODase activity is measured by the DCIP colorimetric assay. This is a coupled assay in which oxidation of DHO and subsequent reduction of ubiquinone are stoichiometrically equivalent to the reduction of DCIP. Reduction of DCIP is accompanied by a loss of absorbance at 610 nm (ε=21500 M/cm). The assay is performed in a 96-well microtiter plate at ambient temperature (ca. 25°C). Stock solutions of 10 mM leflunomide and A771726 are prepared in dimethyl sulfoxide (DMSO) and these are diluted with reaction buffer (100 mM Tris and 0.1 % Triton X-100, pH 8.0) to prepare working stocks of the inhibitors at varying concentrations. For each reaction, the well contained 10 nM DHODase, 68 μM DCIP, 0.16 mg/mL gelatin, the stated concentration of ubiquinone, 10 μL of an inhibitor working stock to give the stated final concentration, and reaction buffer. After a 5-min equilibration period, the reaction is initiated by addition of DHO to the stated final concentrations. The total volume of reaction mixture for each assay is 150 μL, and the final DMSO concentration is ≤ 0.01% (v/v). The reaction progress is followed by recording the loss of absorbance at 610 nm over a 10-min period (during which the velocity remained linear). Velocities are reported as the change in absorbance at 610 nm per minute, and each reported value is the average of three replicates. In experiments where the DHO or ubiquinone concentration is varied, the other substrate is held constant at 200 μM. To determine the inhibitor potency of leflunomide and A771726, the effects of varying concentrations of the two compounds on the initial velocity of the DHODase reaction is measured over a concentration range of 0.01−1.0 μM. In these experiments the DHO and ubiquinone concentrations are held constant at 200 and 100 μM, respectively.

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

    • [1]. Davis JP, et al. The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase. Biochemistry. 1996 Jan 30;35(4):1270-3.  [Content Brief]

      [2]. Xu X, et al. Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide. J Biol Chem. 1995 May 26;270(21):12398-403.  [Content Brief]

      [3]. Fox RI, et al. Mechanism of action for leflunomide in rheumatoid arthritis. Clin Immunol. 1999 Dec;93(3):198-208.  [Content Brief]

    • [1]. Davis JP, et al. The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase. Biochemistry. 1996 Jan 30;35(4):1270-3.

      [2]. Xu X, et al. Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide. J Biol Chem. 1995 May 26;270(21):12398-403.

      [3]. Fox RI, et al. Mechanism of action for leflunomide in rheumatoid arthritis. Clin Immunol. 1999 Dec;93(3):198-208.

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.7008 mL 18.5041 mL 37.0083 mL 92.5206 mL
    5 mM 0.7402 mL 3.7008 mL 7.4017 mL 18.5041 mL
    10 mM 0.3701 mL 1.8504 mL 3.7008 mL 9.2521 mL
    15 mM 0.2467 mL 1.2336 mL 2.4672 mL 6.1680 mL
    20 mM 0.1850 mL 0.9252 mL 1.8504 mL 4.6260 mL
    25 mM 0.1480 mL 0.7402 mL 1.4803 mL 3.7008 mL
    30 mM 0.1234 mL 0.6168 mL 1.2336 mL 3.0840 mL
    40 mM 0.0925 mL 0.4626 mL 0.9252 mL 2.3130 mL
    50 mM 0.0740 mL 0.3701 mL 0.7402 mL 1.8504 mL
    60 mM 0.0617 mL 0.3084 mL 0.6168 mL 1.5420 mL
    80 mM 0.0463 mL 0.2313 mL 0.4626 mL 1.1565 mL
    100 mM 0.0370 mL 0.1850 mL 0.3701 mL 0.9252 mL
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    • Metabolic Enzyme/Protease Anti-infection
    • Dihydroorotate Dehydrogenase Endogenous Metabolite Bacterial
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    • 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.

    Keywords:

    Leflunomide75706-12-6HWA486 RS-34821 SU101HWA 486HWA-486RS34821RS 34821RS-34821SU101SU 101SU-101Dihydroorotate DehydrogenaseEndogenous MetaboliteBacterialDHODHInhibitorinhibitorinhibit

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