Triptolide

Biological Activity

Triptolide inhibits DNA-dependent ATPase activity of XBP and induces inhibition of RNA polymerase II (RNAPII)-mediated transcription (IC₅₀ = 200 nM). Selective for RNAPII over RNAPI and RNAPIII. Triptolide blocks RNA synthesis in HeLa cells (IC₅₀ = 62 nM); exhibits potent antiproliferative activity in 60 cancer cell lines (average IC₅₀ = 12 nM) and induces apoptosis by blocking TNF-α-mediated c-IAP1 and c-IAP2 induction. Also displays immunosuppressive and anti-inflammatory activity.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Defining the location of promoter-associated R-loops at near-nucleotide resolution using bisDRIP-seq
   JG Dumelie, SR Jaffrey
   Elife, 2017;6(0):.
2. Anti-inflammatory Effects of Mapracorat, a Novel Selective Glucocorticoid Receptor Agonist, Is Partially Mediated by MAP Kinase Phosphatase-1 (MKP-1).
   Vollmer T, Stockhausen A, Zhang J
   J Biol Chem, 2012;287(42):35212-21.
3. XPB, a subunit of TFIIH, is a target of the natural product triptolide.
   Titov et al.
   Nat.Chem.Biol., 2011;7:182
4. Immunosuppressant PG490 (Triptolide) inhibits T-cell interleukin-2 expression at the level of purine-box/nuclear factor of activated T-cells and NF-κB transcriptional activation.
   Qui et al.
   J.Biol.Chem., 1999;274:13443
5. PG490 (Triptolide) cooperates with tumor necrosis factor-α to induce apoptosis in tumor cells.
   Lee et al.
   J.Biol.Chem., 1999;274:13451

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