Triptolide

Catalog No.S3604 Batch:S360405

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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
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.)

Preparing Stock Solutions

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)

References

  • https://pubmed.ncbi.nlm.nih.gov/10224109/
  • https://pubmed.ncbi.nlm.nih.gov/12533674/
  • https://pubmed.ncbi.nlm.nih.gov/10224110/
  • https://pubmed.ncbi.nlm.nih.gov/17360534/
  • https://pubmed.ncbi.nlm.nih.gov/23583804/

Customer Product Validation

Spironolactone (sp.) and triptolide inhibit NER in myeloma cells. RPMI8226 cells were incubated with dimethyl sulfoxide (DMSO), spironolactone (10 μm) or triptolide (1 μm) for 6 h before NER evaluation. The figure represents the persistence of DNA-damage signal 150 min after exposure to UV (AFU: arbitrary fluorescent unit). Figure 4a shows representative merged pictures of DAPI and DDB2 proteo-probe signal (b).

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

Treatment with triptolide selectively induces apoptosis of cultured and primary CD19+ CLL cells. A. Percent apoptosis (Annexin V-FITC and PI staining) in Mec-1, Mec-2 and WAC3-CD5+ cells exposed to the indicated doses of triptolide for 48 hrs; bars indicate standard deviation. B. Percent apoptosis of CD19+ normal and primary CLL (both high and low risk) cells exposed to the indicated doses of triptolide for 48 hrs; bars indicate standard deviation. C. Percent of WaC3-CD5+ and Mec-1 cells in different phases of the cell cycle (G0/G1, S and G2/M) exposed to the indicated doses of triptolide for 24 hrs. D. Immunoblot analyses of HSF1, HSP70, cleaved caspase-3 and β-actin obtained from the cell lysates of CD19+ primary CLL cell samples treated with the indicated doses of triptolide for 24 hrs.

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

Triptolide decreases the levels of XRCC1, PARP1 and RAD51. (A) After treatment with 30 nM triptolide for 24 h, western blot assay shows triptolide decreases the levels of XRCC1, PARP1 and slightly influences the levels of RAD51. The assay was repeated in triplicate. (B) The quantification of western blot assay was analyzed. t-test, ***p < 0.001, **p < 0.01 vs the control group.

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

Triptolide inhibited the growth, viability and ACTH secretion of AtT20 cells. (A) AtT20 cells were treated with increasing doses of triptolide. Cell growth was determined by CCK8 assay after 96 h. The data were quantified as% of vehicle (0.01% DMSO). (B) AtT20 cells were treated with increasing doses of triptolide for 96 h. Cells were trypsinized and counted. The data were calculated as% of vehicle control. (C) AtT20 cells were treated with indicated doses of triptolide for 14–21 days. The colonies were visualized by crystal violet staining and quantified in 4 random fields each well. The average number of colonies were calculated and presented as% of vehicle control. (D) AtT20 cells were treated with 100 nM triptolide for 24 h, 48 h, 72 h and 96 h respectively. Cell growth was determined by CCK8 assay. The data were calculated as% of corresponding vehicle control. (E) Cells were treated with indicated doses of triptolide for 24 h. Effects of triptolide on Pomc mRNA expression were assessed by real-time PCR, using β-actin as a control. (F) Cells were treated with indicated doses of triptolide for 24 h. Equal amount of the cell culture supernatants were used for hormone measurement by competitive-ELISA, ACTH secreting levels were calculated according to the standard reference provided by the company. Data were normalized with the number of cells. All Data were presented as means ± SD of three independent experiments each performed with at least quadruplicates. *P < 0.05; **P < 0.01. vs control.

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

Selleck's Triptolide has been cited by 48 publications

Chromatin-bound U2AF2 splicing factor ensures exon inclusion [ Mol Cell, 2025, S1097-2765(25)00316-8] PubMed: 40315850
Chromosomal tethering and mitotic transcription promote ecDNA nuclear inheritance [ Mol Cell, 2025, 85(15):2839-2853.e8] PubMed: 40614723
Triptolide targets PPP2CA/ITGA5 axis to suppress lactate-driven ovarian cancer progression [ Chin Med, 2025, 20(1):122] PubMed: 40770810
Triptolide and its prodrug Minnelide target high-risk MYC-amplified medulloblastoma in preclinical models [ J Clin Invest, 2024, 134(15)e171136] PubMed: 38885332
Dormant cancer cells and polyploid giant cancer cells: The roots of cancer recurrence and metastasis [ Clin Transl Med, 2024, 14(2):e1567] PubMed: 38362620
HIRA protects telomeres against R-loop-induced instability in ALT cancer cells [ Cell Rep, 2024, 43(11):114964] PubMed: 39509271
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
Triptolide, a Cancer Cell Proliferation Inhibitor, Causes Zebrafish Muscle Defects by Regulating Notch and STAT3 Signaling Pathways [ Int J Mol Sci, 2024, 25(9)4675] PubMed: 38731894

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