| Assay Method Information | |
| | Pyridine Analogs Inhibit NO Production |
| Description: | Because oxidative and inflammatory stress contribute to carcinogenesis (Albini & Sporn (2007) Nature Rev. Cancer 7:139-147), it was determined whether the pyridine analogues could block de novo synthesis of inducible nitric oxide synthase (iNOS), a critical enzyme involved in the inflammatory response (Kroncke, et al. (1998) Clin. Exp. Immunol. 113:147-156; Zamora, et al. (2000) Mol. Med. 6:347-373). Nitric oxide release was determined in RA W264.7 macrophage-like cells, after stimulation with 10 ng/ml interferon-γ (IFNγ) and a 24 hour-exposure to each compound at 0.625, 1.3, 2.5, 5, 10 and 20 nM. NO release was measured by Griess reaction and compared to CDDO-Im, which is a potent suppressor of iNOS (Place, et al. (2003) Clin. Cancer Res. 19:2798-2806). This analysis indicated that the new analogues were slightly less potent than CDDO-Im for blocking NO production. However, each analog inhibited NO production in the low nanomolar range with IC50 values between 2-15 nM (Table 2). The order of potency in the NO assay was similar to the results obtained in the U937 differentiation assay with CDDO-Im (2.0 nM) and CDDO-3P-Im (4.3 nM) being the most active and CDDO-Phenyl-Im being the least active (14.7 nM). |
| Affinity data for this assay | |
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