Rocaglamide

Rocaglamide is a potent inhibitor of NFkB in T-lymphocytes with almost complete inhibition at 200nM.1 It was able to completely inhibit IL-4 and IFN-γ production and suppress 60-85% of IL-2 and TNF-α production at 50nM in T-cells without inhibiting AP-1 and NF-kB (conversely, at concentrations <100nM, it was shown to increase NF-kB activity) .2 Immunosuppression activity was due to inhibition of cytokine gene expression via blocking of NF-AT activity and is a different mechanism than suppression via Cyclosporine a and FK-506. Rocaglamide has anti-cancer properties via various pathways including ERK inhibition3, ATM/ATR-Chk1/Chk2 activation4, and p38 and JNK activation5.