NFAT Transcription Factor Regulator is an IL-2 synthesis inhibitor with an IC50 of 182 nM.
NFAT Transcription Factor Regulator is compound example 19. NFAT Transcription Factor Regulator inhibits IL-2 synthesis with an IC50 of 182 nM. It inhibits human and rat PBMC proliferation with IC50s of 82 and 146 nM, respectively. It is able to inhibit IL-4 and IL-5 production in human T-cell lines with similar potency to its effects on IL-2 release[1].
NFAT Transcription Factor Regulator is found to have an inhibitory potency approximately 10-fold better than that of cyclosporine. Comparable inhibitory effects on T-cell IL-2 production are obtained with NFAT Transcription Factor Regulator and cyclosporine at doses of 3.0 and 30 mg/kg, po, respectively. The efficacies achieved in monkeys in vivo for blocking T-cell cytokine production suggest that NFAT Transcription Factor Regulator has potential similar to that of cyclosporine for use in transplantation[1].
[1]. Djuric SW, et al. 3,5-Bis(trifluoromethyl)pyrazoles: a novel class of NFAT transcription factor regulator. J Med Chem. 2000 Aug 10;43(16):2975-81.