受注:045-509-1970 |
技術サポート:[email protected] 平日9:00〜18:00 1営業日以内にご連絡を差し上げます |
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. |
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. 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] |
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]
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 |
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 |
Bruceine A protects against diabetic kidney disease via inhibiting galectin-1 [ Kidney Int, 2022, S0085-2538(22)00369-6] | PubMed: 35598813 |
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。