Rocaglamide
TNF-α inhibitor / 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.
Biochemicals & reagents
84573-16-0
RocA
1) Baumann et al. (2002), Rocaglamide Derivatives Are Potent Inhibitors of NF-kB Activation in T-cells; J.Biol.Chem. 277 44791 2) Prolsch et al. (2005), Rocaglamide Derivativews Are Immunosuppressive Phytochemicals That Target NF-AT Activity in T Cells; J.Immunol. 174 7075 3) Polier et al. (2012), The natural anticancer compounds rocaglamides inhibit the Raf-MEK-ERK pathway by targeting prohibitin1 and 2; Chem.Biol. 19 1093 4) Neumann et al. (2014), The natural anticancer compound rocaglamide selectively inhibits the G1-S phase transition in cancer cells through the ATM/ATR-mediated Chk1/2 cell cycle checkpoints; Int.J.Cancer 134 1991 5) Zhu et al. (2007), The traditional Chinese herbal compound rocaglamide preferentially induces apoptosis in leukemia cells by modulation of mitogen-activated protein kinase activities; Int.J.Cancer 121 1839
-20°C
PATHWAY: TNF; NFkappaB; Protein synthesis; Cytokine; DNA damage; Transcription -- RESEARCH AREA: Immunology -- DISEASE AREA: Inflammation; Cancer