Triptolide

製品コードS3604 バッチS360407

印刷

化学情報

Chemical Structure Synonyms PG490, NSC 163062 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H24O6
分子量 360.4 CAS No. 38748-32-2
Solubility (25°C)* 体外 DMSO 72 mg/mL warmed with 50ºC water bath (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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
in vitro Triptolide is a diterpene triepoxide with potent immunosuppressive and antiinflammatory properties. This compound 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] It inhibits the proliferation and colony formation of tumor cells at extremely low concentrations (2–10 ng/mL). This chemical has an inhibitory activity on breast, stomach and leukemia cell line HL-60 cells. It 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] This compound 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, it inhibits experimental metastasis of B16F10 cells to the lungs and spleens of mice. [2] It has in vitro and in vivo activities against mouse models of polycystic kidney disease. [4] LD50: Mice 0.83mg/kg (i.v.). [5]

プロトコル(参考用のみ)

参考

  • 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/

カスタマーフィードバック

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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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
The functional organization of chromosome territories in single nuclei during zygotic genome activation [ bioRxiv, 2025, 2025.04.06.647428] PubMed: 40994625
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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。