Biochemicals & reagents
1) He et al. (2015), Covalent Modification of a Cysteine Residue in the XPB Subunit of the General Transcription Factor TFIIH Through Single Epoxide Cleavage of the Transcription Inhibitor Triptolide; Angew.Chem.Int.Ed.Eng. 54 1859 2) Lee et al. (1999), PG490 (Triptolide) Cooperates with Tumor Necrosis factor-α to Induce Apoptosis in Tumor Cells; J.Biol.Chem, 274 13451 3) Qiao et al. (2016), Synergistic antitumor activity of gemcitabine combined with triptolide in pancreatic cancer cells; Oncol.Lett., 11 3527 4) Fan et al. (2016), Triptolide Modulates TREM-1 Signal Pathway to Inhibit the Inflammatory Response in Rheumatoid Arthritis; Int.J.Mol.Sci. 17 498
Triptolide possesses a potent immunosuppressive and anti-inflammatory activity and it irreversibly inhibits eukaryotic transcription via covalent binding to XPB, a subunit of the transcription factor TFIIH (1). This compound 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). It also inhibits the inflammatory response and remarkably decreases production of TNF-α, IL-1β and IL-6 in a rat model of rheumatoid arthritis (4).