Triptolide

A potent immunosuppressive and anti-inflammatory agent. Irreversibly inhibits eukaryotic transcription via covalent binding to XPB, a subunit of the transcription factor TFIIH [1]. Blocks transactivation of NFκB [2]. Exhibits potent antiproliferative activity in 60 cancer cell lines (average IC50 = 12 nM) and synergizes with other anticancer agents [3]. Inhibits the inflammatory response and remarkably decreases production of TNF-α, IL-1β and IL-6 in a rat model of rheumatoid arthritis [4]. A fast acting RNA polymerase II inhibitor [5].

References:

1) QL He et al. Angew. Chem. Int. Ed. Eng. 2015 54:1859

2) KY Lee et al. J. Biol. Chem. 1999 274:13451

3) Z Qiao et al. Oncol. Lett. 2016 11:3527

4) D Fan et al. Int. J. Mol. Sci. 2016 17:498

5) S Vispe et al. Mol. Cancer Ther. 2009 8:2780