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Triptolide Hsp90 Middle Domain Inhibitor

Name: Triptolide
Brand: Selleck Chemicals
SKU: S3604
Availability: InStock
Rating: 5 (47 reviews)

Cat.No.S3604

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.

Chemical Structure

Molecular Weight: 360.4

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Quality Control

Batch: Purity: 99.95%

99.95

Related Targets	NF-κB HDAC Antioxidant ROS IκB/IKK Nrf2 AP-1 MALT NOD
Other ADC Cytotoxin Inhibitors	SN-38 (+)-Bicuculline Rutin Artemisinin Pinocembrin BHQ Harmine hydrochloride Psoralen Lappaconite HBr Luteoloside

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 72 mg/mL (199.77 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
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.
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.
Clear solution	2%DMSO 1 30%PEG300 2 2%Tween80 3 66%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.000mg/ml (8.32mM)	Taking the 1 mL working solution as an example, add 20 μL of 150 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 660 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
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.
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.

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: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	360.4	Formula	C₂₀H₂₄O₆	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	38748-32-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

Targets/IC₅₀/Ki	NF-κB HSF1 MDM2
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. 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.
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. 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. It has in vitro and in vivo activities against mouse models of polycystic kidney disease. LD50: Mice 0.83mg/kg (i.v.).
References	[1] https://pubmed.ncbi.nlm.nih.gov/10224109/ [2] https://pubmed.ncbi.nlm.nih.gov/12533674/ [3] https://pubmed.ncbi.nlm.nih.gov/10224110/ [4] https://pubmed.ncbi.nlm.nih.gov/17360534/ [5] https://pubmed.ncbi.nlm.nih.gov/23583804/

Applications

Methods	Biomarkers	Images	PMID
Western blot	c-Jun MDM2 p-AKT / AKT / p-Foxo3a / Foxo3a / p53 p-PI3K / PI3K / p85 / p110		22666381
Growth inhibition assay	Cell viability		22666381

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