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Submit ReviewTriptolide
Description: Inhibits RNAPII-mediated transcription; antitumor, anti-inflammatory and immunosuppressive
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
Purity: ≥98% (HPLC)
Biological Activity for Triptolide
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.
Compound Libraries for Triptolide
Triptolide is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Antiviral Library and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for Triptolide
| M. Wt | 360.4 |
| Formula | C20H24O6 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 38748-32-2 |
| PubChem ID | 107985 |
| InChI Key | DFBIRQPKNDILPW-CIVMWXNOSA-N |
| Smiles | O=C1C2=C([C@@](C[C@H]5[C@]4(O5)[C@](O6)3[C@@H]6[C@H]7[C@](C(C)C)(O7)[C@H]4O)([H])[C@]3(C)CC2)CO1 |
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.
Solubility Data for Triptolide
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 7.21 | 20 |
Preparing Stock Solutions for Triptolide
The following data is based on the product molecular weight 360.4. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 13.87 mL | 69.37 mL | 138.73 mL |
| 1 mM | 2.77 mL | 13.87 mL | 27.75 mL |
| 2 mM | 1.39 mL | 6.94 mL | 13.87 mL |
| 10 mM | 0.28 mL | 1.39 mL | 2.77 mL |
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Product Datasheets for Triptolide
References for Triptolide
References are publications that support the biological activity of the product.
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
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
Titov et al (2011) XPB, a subunit of TFIIH, is a target of the natural product triptolide. Nat.Chem.Biol. 7 182 PMID: 21278739
If you know of a relevant reference for Triptolide, please let us know.
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Keywords: Triptolide, Triptolide supplier, Blocks, TNF-α, TNF-alpha-mediated, c-IAP2, c-IAP1, induction, inhibitors, inhibits, apoptosis, TNF-alpha-induced, NF-κB, NF-kappaB, NF-kB, activation, X-Linked, Apoptosis, XIAP, Nuclear, Factor, Kappa, B, Cytokine, Signaling, Signalling, Transcription, Factors, Immunosuppressants, DNA, Polymerase, RNA, DNA,, and, Protein, Synthesis, Inhibitor, of, (IAP), 3253, Tocris Bioscience
8 Citations for Triptolide
Citations are publications that use Tocris products. Selected citations for Triptolide include:
Shao et al (2019) Reporter-ChIP-nexus reveals strong contribution of the Drosophila initiator sequence to RNA polymerase pausing. Elife 8 PMID: 31021316
Tettey et al (2019) A Role for FACT in RNA Polymerase II Promoter-Proximal Pausing. Cell Rep 27 3770 PMID: 31242411
Vollmer et al (2012) Anti-inflammatory effects of mapracorat, a novel selective glucocorticoid receptor agonist, is partially mediated by MAP kinase phosphatase-1 (MKP-1). J Biol Chem 287 35212 PMID: 22898817
Bowry et al (2018) BET Inhibition Induces HEXIM1- and RAD51-Dependent Conflicts between Transcription and Replication. Cell Rep 25 2061 PMID: 30463005
Filone et al (2014) The master regulator of the cellular stress response (HSF1) is critical for orthopoxvirus infection. PLoS Pathog 10 e1003904 PMID: 24516381
Petropoulos et al (2024) Transcription-replication conflicts underlie sensitivity to PARP inhibitors. Nature 628 433 PMID: 38509368
Liao and Mizzen (2017) Site-specific regulation of histone H1 phosphorylation in pluripotent cell differentiation. Epigenetics Chromatin 10 29 PMID: 28539972
Zhao et al (2015) Hyaluronic acid prevents immunosuppressive drug-induced ovarian damage via up-regulating PGRMC1 expression. Sci Rep 5 7647 PMID: 25558795
Do you know of a great paper that uses Triptolide from Tocris? Please let us know.
Reviews for Triptolide
Average Rating: 5 (Based on 1 Review.)
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Works well.
By
Anonymous on 06/22/2020
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: U2OS
triptolide (1 μM)
I used short treatments with the transcription inhibitors triptolide. These inhibited ongoing RNA synthesis and increased replication fork speeds specifically in the presence of JQ1
