Home NF-κB ADC Cytotoxin chemical - NF-κB inhibitor - MDM2/MDMX inhibitor - Apoptosis related activator - HSP (HSP90) inhibitor Triptolide For research use only.

Triptolide

Synonyms: PG490, NSC 163062

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.

Triptolide Chemical Structure

Triptolide Chemical Structure

CAS No. 38748-32-2

Purity & Quality Control

Triptolide Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT-29 Cytotoxicity against Cytotoxicity against human HT-29 cells, IC50=0.0021μM 21470864
HCT116 Cytotoxicity against Cytotoxicity against human HCT116 cells assessed as decrease in cell viability, IC50=0.0047μM 31121546
SKOV3 Antiproliferative activity against 72 hrs Antiproliferative activity against human SKOV3 cells after 72 hrs by SRB assay, IC50=0.006μM 20833543
SKOV3 Cytotoxicity against 72 hrs Cytotoxicity against human SKOV3 cells after 72 hrs by sulforhodamine B assay, IC50=0.006μM 24378709
SKOV3 Cytotoxic activity against 72 hrs Cytotoxic activity against human SKOV3 cells assessed as reduction in cell viability after 72 hrs by SRB assay, IC50=0.0072μM 28011223
KBM5 Cytotoxicity against 72 hrs Cytotoxicity against imatinib-resistant human KBM5 cells harboring Bcr-Abl T315I mutant after 72 hrs by MTS assay, IC50=0.0083μM 20149665
SKOV3 Cytotoxicity against Cytotoxicity against human SKOV3 cells by SRB assay, IC50=0.009μM 19637874
MDA-MB-468 Cytotoxicity against Cytotoxicity against human MDA-MB-468 cells by SRB assay, IC50=0.01μM 19637874
HCT116 Cytotoxicity against 72 hrs Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.01μM 19637874
SKOV3 Cytotoxicity against 72 hrs Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay, IC50=0.01μM 19637874
KBM5 Cytotoxicity against 72 hrs Cytotoxicity against human KBM5 cells harboring wild type Bcr-Abl after 72 hrs by MTS assay, IC50=0.0103μM 20149665
Rh30 Cytotoxicity against 72 hrs Cytotoxicity against human Rh30 cells after 72 hrs by MTT assay, IC50=0.014μM 19637874
A549 Antagonist activity at Antagonist activity at human PAR2 expressed in human A549 cells assessed as inhibition of 2f-LIGRLO-NH2-induced NFkappaB activation by luciferase reporter gene assay, IC50=0.014μM 23895492
SGC7901 Cytotoxicity against 72 hrs Cytotoxicity against human SGC7901 cells after 72 hrs by MTT assay, IC50=0.015μM 19637874
MOLT4 Cytotoxicity against 72 hrs Cytotoxicity against human MOLT4 cells after 72 hrs by MTT assay, IC50=0.017μM 19637874
A549 Cytotoxic activity against 72 hrs Cytotoxic activity against human A549 cells assessed as reduction in cell viability after 72 hrs by SRB assay, IC50=0.0175μM 28011223
SMMC7721 Cytotoxicity against 72 hrs Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay, IC50=0.018μM 19637874
PC3 Cytotoxic activity against 72 hrs Cytotoxic activity against human PC3 cells assessed as reduction in cell viability after 72 hrs by SRB assay, IC50=0.0183μM 28011223
MCF7 Cytotoxicity against 72 hrs Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay, IC50=0.019μM 19637874
A549 Cytotoxicity against Cytotoxicity against human A549 cells, IC50=0.019μM 21470864
PC3 Cytotoxicity against Cytotoxicity against human PC3 cells by SRB assay, IC50=0.02μM 19637874
Bel7402 Cytotoxicity against 72 hrs Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay, IC50=0.02μM 19637874
PC3 Antiproliferative activity against 72 hrs Antiproliferative activity against human PC3 cells after 72 hrs by SRB assay, IC50=0.02μM 20833543
PC3 Cytotoxicity against 72 hrs Cytotoxicity against human PC3 cells after 72 hrs by sulforhodamine B assay, IC50=0.02μM 24378709
PC3 Cytotoxicity against Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation by sulforhodamine B assay, IC50=0.02μM 25467158
786-O Cytotoxicity against 72 hrs Cytotoxicity against human 786-O cells after 72 hrs by MTT assay, IC50=0.022μM 19637874
A549 Antagonist activity at Antagonist activity at human PAR2 expressed in human A549 cells coexpressing TACR1 assessed as inhibition of substance P-induced IL-8 production by ELISA, IC50=0.023μM 23895492
MDA-MB-231 Cytotoxicity against 72 hrs Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50=0.024μM 19637874
DU145 Cytotoxicity against 72 hrs Cytotoxicity against human DU145 cells after 72 hrs by MTT assay, IC50=0.024μM 19637874
HO8910 Cytotoxicity against 72 hrs Cytotoxicity against human HO8910 cells after 72 hrs by MTT assay, IC50=0.028μM 19637874
HCT15 Cytotoxicity against 72 hrs Cytotoxicity against human HCT15 cells after 72 hrs by MTT assay, IC50=0.029μM 19637874
A549 Growth inhibition of human Growth inhibition of human A549 cells, IC50=0.03μM 28814374
32D Cytotoxicity against 72 hrs Cytotoxicity against mouse 32D cells harboring wild type Bcr-Abl after 72 hrs by MTS assay, IC50=0.032μM 20149665
U251 Cytotoxicity against Cytotoxicity against human U251 cells assessed as inhibition of cell proliferation by sulforhodamine B assay, IC50=0.033μM 25467158
32D Cytotoxicity against 72 hrs Cytotoxicity against imatinib-resistant mouse 32D cells harboring Bcr-Abl T315I mutant after 72 hrs by MTS assay, IC50=0.034μM 20149665
PC3 Cytotoxicity against 72 hrs Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50=0.043μM 19637874
KB Cytotoxicity against 72 hrs Cytotoxicity against human KB cells after 72 hrs by MTT assay, IC50=0.043μM 19637874
HepG2 Cytotoxicity against 48 hrs Cytotoxicity against human HepG2 cells after 48 hrs by XTT assay, IC50=0.0433μM 30613335
HeLa Cytotoxicity against 72 hrs Cytotoxicity against human HeLa cells after 72 hrs by MTT assay, IC50=0.047μM 19637874
U251 Cytotoxicity against 72 hrs Cytotoxicity against human U251 cells after 72 hrs by MTT assay, IC50=0.049μM 19637874
K562 Cytotoxicity against 72 hrs Cytotoxicity against human K562 cells after 72 hrs by MTT assay, IC50=0.05μM 19637874
NIH/3T3 Cytotoxicity against Cytotoxicity against mouse NIH/3T3 cells assessed as decrease in cell viability, IC50=0.05μM 31121546
SW1116 Cytotoxicity against 72 hrs Cytotoxicity against human SW1116 cells after 72 hrs by MTT assay, IC50=0.052μM 19637874
A549 Cytotoxicity against 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=0.059μM 19637874
HeLa Cytotoxicity against Cytotoxicity against human HeLa cells assessed as decrease in cell viability, IC50=0.087μM 31121546
Jurkat Cytotoxicity against Cytotoxicity against human Jurkat cells assessed as decrease in cell viability, IC50=0.14μM 31121546
MKN28 Cytotoxicity against 72 hrs Cytotoxicity against human MKN28 cells after 72 hrs by MTT assay, IC50=0.2μM 19637874
MDCK Cytotoxicity against Cytotoxicity against MDCK cells assessed as decrease in cell viability, IC50=1.2μM 31121546
Pkd1-/- Induction of Induction of cell growth arrest in mouse Pkd1-/- cells in presence of calcium 17360534
Pkd1-/- Increase in 100 nM 96 hrs Increase in p21CIP/WAF expression in mouse Pkd1-/- cells at 100 nM after 96 hrs by Western blot analysis 17360534
Pkd1+/- Increase in 100 nM Increase in PC2 dependent calcium release in mouse Pkd1+/- cells at 100 nM 17360534
Pkd1-/- Increase in 100 nM Increase in PC2 dependent calcium release in mouse Pkd1-/- cells at 100 nM 17360534
Pkd1-/- Increase in 50 uM Increase in calcium release in mouse Pkd1-/- cells at 50 uM in presence of RyR antagonist dantrolene 17360534
Pkd2+/- Growth inhibition of PC2 expressing mouse 100 nM 24 hrs Growth inhibition of PC2 expressing mouse Pkd2+/- cells as cell death at 100 nM after 24 hrs 17360534
KBM5 Cytotoxicity against 0.001 to 17 uM 72 hrs Cytotoxicity against human KBM5 cells harboring wild type Bcr-Abl at 0.001 to 17 uM after 72 hrs by MTS assay 20149665
KBM5 Cytotoxicity against 0.001 to 17 uM 72 hrs Cytotoxicity against imatinib-resistant human KBM5 cells harboring Bcr-Abl T315I mutant at 0.001 to 17 uM after 72 hrs by MTS assay 20149665
LNCAP Antagonist activity at 5 uM 24 hrs Antagonist activity at AR in human LNCAP cells assessed as suppression of DHT-induced receptor transcriptional activity at 5 uM after 24 hrs by dual luciferase reporter gene assay 27994731
LNCAP Antagonist activity at 500 nM 24 hrs Antagonist activity at AR in human LNCAP cells assessed as suppression of DHT-induced receptor transcriptional activity at 500 nM after 24 hrs by dual luciferase reporter gene assay 27994731
HepG2 Antitumor activity against 0.2 mg/kg 15 days Antitumor activity against human HepG2 cells xenografted in Balb/c nude mouse assessed as reduction in tumor growth at 0.2 mg/kg, ip administered once daily for 15 days 30613335
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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
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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-PI3K / PI3K / p85 / p110 p-AKT / AKT / p-Foxo3a / Foxo3a / p53 MDM2 c-Jun 27004407
Growth inhibition assay Cell viability 22666381
In Vivo
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]

Chemical Information & Solubility

Molecular Weight 360.4 Formula

C20H24O6
CAS No. 38748-32-2 SDF Download Triptolide SDF
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 72 mg/mL ( (199.77 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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