Triptolide

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Cat.No. 3253 - Triptolide | C20H24O6 | CAS No. 38748-32-2
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)
Datasheet
Citations (7)
Reviews (1)
Literature (1)

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.

Compound Libraries

Triptolide is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 7.21 20

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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References

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.

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

7 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

Bowry et al (2018) BET Inhibition Induces HEXIM1- and RAD51-Dependent Conflicts between Transcription and Replication. Cell Rep 25 2061 PMID: 30463005

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


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

PMID: 30463005
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Literature in this Area

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