Triptolide | Immunosuppressant

Triptolide (38748-32-2) possesses potent immunosuppressive and anti-inflammatory activity.  Irreversibly inhibits eukaryotic transcription via covalent binding to XPB, a subunit of the transcription factor TFIIH.¹  Blocks transactivation of NFkB.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-a, IL-1b and IL-6 in a rat model of rheumatoid arthritis.⁴

References/Citations

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