TriptolideCat. No. 3253 |
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Chemical Name: (3bS,4aS,5aS,6R,6aR,7aS,7bS,8aS,8bS)-3b,4,4a,6,6a,7a,7b,8b,9,10-Decahydro-6-hydroxy-8b-methyl-6a-(1-methylethyl)trisoxireno[4b,5:6,7:8a,9]phenanthro[1,2-c]furan-1(3H)-one |
Biological Activity
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. 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.Certificate of Analysis / Safety Data Sheet
References
Lee et al (1999) PG490 (Triptolide) cooperates with tumor necrosis factor-α to induce apoptosis in tumor cells. J.Biol.Chem. 274 13451. PMID: 10224110.
Qui et al (1999) 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. J.Biol.Chem. 274 13443. PMID: 10224109.
Titov et al (2011) XPB, a subunit of TFIIH, is a target of the natural product triptolide. Nat.Chem.Biol. 7 182. PMID: 21278739.
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Keywords: Triptolide, supplier, Blocks, TNF-α, TNF-alpha-mediated, c-IAP2, c-IAP1, induction, inhibitors, apoptosis, TNF-alpha-induced, NF-κB, NF-kappaB, NF-kB, activation, X-Linked, Apoptosis, XIAP, Nuclear, Factor, Kappa, B, Cytokine, Signaling, Signalling, Transcription, Factors
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