Triptolide

Catalog No.S3604 Batch:S360404

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Technical Data

Formula

C20H24O6
Molecular Weight 360.4 CAS No. 38748-32-2
Solubility (25°C)* In vitro DMSO 72 mg/mL (199.77 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Triptolide is a diterpene triepoxide, immunosuppresive agent extracted from the Chinese herb Tripterygium wilfordii. It functions as a NF-κB inhibitor with dual actions by disruption of p65/CBP interaction and by reduction of p65 protein. Triptolide (PG490) abrogates the transactivation function of heat shock transcription factor 1 (HSF1). Triptolide inhibits MDM2 and induces apoptosis through a p53-independent pathway.
Targets
NF-κB [1] HSF1 [1] MDM2 [1]
In vitro Triptolide is a diterpene triepoxide with potent immunosuppressive and antiinflammatory properties. Triptolide is shown to inhibit the expression of IL-2 in activated T cells at the level of purine-box/nuclear factor and NF-κB mediated transcription activation. [1] Triptolide inhibits the proliferation and colony formation of tumor cells at extremely low concentrations (2–10 ng/mL). Triptolide has an inhibitory activity on breast, stomach and leukemia cell line HL-60 cells. Triptolide induces apoptosis in tumor cells by blocking NF-κB activation and sensitizing tumor cells for TNF-&alpha induced programmed cell death. [2]
In vivo Triptolide synergizes with cyclosporin A in promoting graft survival in animal models and in suppression of graft versus host disease in allogeneic bone marrow transplants. In addition, it induces apoptosis in tumor cells and potentiates tumor necrosis factor (TNF-α) induction of apoptosis in part through the suppression of c-IAP2 and c-IAP1 induction. [1] [3] Triptolide treatment for 2–3 weeks inhibits the growth of xenografts formed by four different tumor cell lines (B16 melanoma, MDA-435 breast cancer, TSU bladder cancer, and MGC80-3 gastric carcinoma), indicating that TPL has a broad spectrum of activity against tumors that contain both wild-type and mutant forms of p53. In addition, Triptolide inhibits experimental metastasis of B16F10 cells to the lungs and spleens of mice. [2] Triptolide has in vitro and in vivo activities against mouse models of polycystic kidney disease. [4] LD50: Mice 0.83mg/kg (i.v.). [5]

Protocol (from reference)

Customer Product Validation

Data from [Data independently produced by , , Leukemia, 2018, 32(1):111-119]

Data from [Data independently produced by , , Oncotarget, 2015, 6(31):31767-79]

Data from [Data independently produced by , , Biomed Pharmacother, 2019, 109:1541-1546]

Data from [Data independently produced by , , Biomed Pharmacother, 2017, 95:771-779]

Selleck's Triptolide has been cited by 42 publications

Dormant cancer cells and polyploid giant cancer cells: The roots of cancer recurrence and metastasis [ Clin Transl Med, 2024, 14(2):e1567] PubMed: 38362620
Targeted inhibition of the HNF1A/SHH axis by triptolide overcomes paclitaxel resistance in non-small cell lung cancer [ Acta Pharmacol Sin, 2024, 10.1038/s41401-023-01219-y] PubMed: 38228910
DEAD-box helicase 1 inhibited CD8+ T cell antitumor activity by inducing PD-L1 expression in hepatocellular carcinoma [ Cancer Sci, 2024, 10.1111/cas.16076] PubMed: 38243657
DEAD-box helicase 1 inhibited CD8+ T cell antitumor activity by inducing PD-L1 expression in hepatocellular carcinoma [ Cancer Sci, 2024, 115(3):763-776] PubMed: 38243657
APOBEC3B regulates R-loops and promotes transcription-associated mutagenesis in cancer [ Nat Genet, 2023, 55(10):1721-1734] PubMed: 37735199
APOBEC3B regulates R-loops and promotes transcription-associated mutagenesis in cancer [ Nat Genet, 2023, 55(10):1721-1734] PubMed: 37735199
P-TEFb promotes cell survival upon p53 activation by suppressing intrinsic apoptosis pathway [ Nucleic Acids Res, 2023, gkad001] PubMed: 36727434
Astrocyte-derived SerpinA3N promotes neuroinflammation and epileptic seizures by activating the NF-κB signaling pathway in mice with temporal lobe epilepsy [ J Neuroinflammation, 2023, 20(1):161] PubMed: 37422673
Pharmacological inhibition of human EZH2 can influence a regenerative β-like cell capacity with in vitro insulin release in pancreatic ductal cells [ Clin Epigenetics, 2023, 15(1):101] PubMed: 37309004
RNA Polymerase II, the BAF remodeler and transcription factors synergize to evict nucleosomes [ bioRxiv, 2023, 2023.01.22.525083] PubMed: 36711459

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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