NFAT-AP-1 interaction inhibitor 10 (NFAT inhibitor compound 10) is a small-molecule inhibitor nuclear factor of activated T cells (NFAT) with IC50 of 2 uM in FRET assays.
NFAT-AP-1 interaction inhibitor 10 (NFAT inhibitor compound 10) is a small-molecule inhibitor nuclear factor of activated T cells (NFAT) with IC50 of 2 uM in FRET assays.
Compound 10 inhibits production of the cytokines IL-2 and TNF by total CD4+ murine T cells under conditions where it is not toxic to the cells.
NFAT inhibitor compound 10 inhibits formation of the quaternary NFAT:Fos:Jun:DNA complex on the ARRE-2 site, but not on the GM-330 element, without inhibiting the direct binding of NFAT or AP-1 to DNA.
Compound 10 alters the gene expression pattern of stimulated T cells and inhibits the expression of many NFAT-dependent genes, included Il2 and Nfatc1 (encoding NFAT2) short isoform, as well as Cd160, Erg1, and Xcl1, Nfkb1 (encoding NF-κB p50).
