Description
NFAT inhibitor is a cell-
permeable compound that selectively inhibits calcineurin-
mediated dephosphorylation of NFAT. At 100 μM, this inhibitor effectively blocks calcineurin binding to NFAT without disrupting other calcineurin-
dependent pathways, unlike the immunosuppressants cyclosporin A and FK506 which indiscriminately block all calcineurin phosphatase activity. NFAT inhibitor can disrupt NFAT-
dependent expression of IL-
2 and TNF-
α when transfected in Jurak T cells and can prevent the activation and proliferation of T cells both
in vitro (~ 43% at 1 μM using mixed lymphocyte cultures) and
in vivo (10 mg/kg using C3H/HeN mice).
