Triptolide (PG490)

For research use only.

Catalog No.S3604 Synonyms: NSC 163062

22 publications

Triptolide (PG490) Chemical Structure

CAS No. 38748-32-2

Triptolide (PG490, NSC 163062) 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.

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Selleck's Triptolide (PG490) has been cited by 22 publications

Purity & Quality Control

Choose Selective ADC Cytotoxin Inhibitors

Biological Activity

Description Triptolide (PG490, NSC 163062) 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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LNCAP MX7BcpRi\2:waYP0JIFkfGm4aYT5JIF1 M4C5R|UxOCCwTR?= M1\STlI1KGi{cx?= MXvBcpRi\2:waYP0JIFkfGm4aYT5JIF1KEGUIHnuJIh2dWGwIFzOR2FRKGOnbHzzJIF{e2W|c3XkJIF{KHO3cIDy[ZN{cW:wIH;mJGRJXC2rbnT1Z4VlKHKnY3XweI9zKHS{YX7zZ5JqeHSrb37hcEBi[3Srdnn0fUBifCB3MECgcm0h[W[2ZYKgNlQhcHK|IHL5JIR2[WxibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 NH\SOlM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{m5OFc{OSd-Mke5PVQ4OzF:L3G+
HepG2 MX;BcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dB?= MoXPNE4zKG2pL3vn MUSxOUBl[Xm| M4\3cWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldGczKGOnbHzzJJhmdm:pcnHmeIVlKGmwIFLhcIIw[yCwdXTlJI1wfXOnIHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiC2dX3vdkBoem:5dHigZZQhOC5{IH3nM4toNCCrcDDh[I1qdmm|dHXy[YQhd26lZTDkZYltgSCob4KgNVUh\GG7cx?= M3LpOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNkGzN|M2Lz5|ME[xN|M{PTxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
c-Jun; 

PubMed: 22666381     


(C) and (D) Triptolide decreased c-Jun protein level in LNCaP (C) and PC-3 (D) cells in a dose-dependent manner. Cells were treated with indicated dose of Triptolide or Celastrol for 24 h before Western blot analysis. α-tubulin was used as a loading control. 

MDM2; 

PubMed: 27004407     


Western blot assays showing the dose-response and time-course of MDM2 inhibition by triptolide. GAPDH served as an internal control for equal protein loading.

p-AKT / AKT / p-Foxo3a / Foxo3a / p53 ; 

PubMed: 27004407     


Western blot assays showing the inhibitory effect of triptolide on Akt activity. MCF-7 and MDA-MB-468 cells were treated with 50 nM triptolide for different times. Cell extracts were tested by Western blot assay for the expression of MDM2, p53, p21, PUMA, Akt, phosphorylated Akt (S473), Foxo3a and phosphorylated Foxo3a. Phosphorylated Akt and phosphorylated Foxo3a were dramatically decreased following treatment with triptolide. The quantification results are shown on the graphs to the right. 

p-PI3K / PI3K / p85 / p110 ; 

PubMed: 27004407     


Triptolide up-regulates p85 expression. MDA-MB-468 cells were treated with 50 nM triptolide for different times. Cell extracts were tested by Western blot assay for the expression of PI3K, phosphorylated PI3K, p85, p110 and REST.

22666381 27004407
Growth inhibition assay
Cell viability; 

PubMed: 22666381     


(C) Effect of Triptolide on LNCaP cells. (E) Effect of Triptolide on PC-3 cells.

22666381
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

Solubility (25°C)

In vitro DMSO 72 mg/mL warmed (199.77 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
3mg/mL

* 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.

Chemical Information

Molecular Weight 360.4
Formula

C20H24O6

CAS No. 38748-32-2
Storage powder
in solvent
Synonyms NSC 163062
Smiles CC(C)C12C(O1)C3C4(O3)C5(CCC6=C(C5CC7C4(C2O)O7)COC6=O)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
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% DMSO % % Tween 80 % ddH2O
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Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID