Cat. No.: HY-N0475

Triptophenolide

(Synonyms: Hypolide; (+)-Triptophenolide)

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Based on 1 Customer Validation

Triptophenolide (Hypolide) is a colorless crystal isolated from the ethyl acetate extract of Tripterygium wilfordii. Triptophenolide is an orally active pan‑antagonist of the androgen receptor (AR) with an IC₅₀ of 467 nM against human wild‑type AR. Triptophenolide reduces AR expression, inhibits AR nuclear translocation, downregulates prostate‑specific antigen mRNA levels, and suppresses the growth of AR‑positive prostate cancer cells. Triptophenolide shows anti-tumor effects against breast cancer by inhibiting cell proliferation and migration, inducing G1-phase arrest and apoptosis, repressing xenograft tumor growth. Triptophenolide inhibits pyroptosis, alleviates tissue inflammation, and ameliorates synovial injury. Triptophenolide can be used for the study of prostate cancer, rheumatoid arthritis and breast cancer.

For research use only. We do not sell to patients.

Purity: 99.98%
CAS No.: 74285-86-2
Formula: C₂₀H₂₄O₃
Molecular Weight:312.40

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Triptophenolide Chemical Structure

CAS No.: 74285-86-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

Caspase 3

Caspase-9

Bax

Bak

Bim

All Caspase Isoforms :

All Bcl-2 Family Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	>60 μM Compound: Triptophenolide	Cytotoxicity against human A2780 cells assessed as cell viability measured after 48 hrs by MTT assay Cytotoxicity against human A2780 cells assessed as cell viability measured after 48 hrs by MTT assay	[PMID: 38964974]
A549	IC₅₀	>100 μM Compound: 43	Cytotoxic activity against human A549 cells assessed as reduction in cell viability after 72 hrs by SRB assay Cytotoxic activity against human A549 cells assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 28011223]
A549	IC₅₀	42.88 μM Compound: 15	Cytotoxicity against human A549 cells after 48 hrs by MTT assay Cytotoxicity against human A549 cells after 48 hrs by MTT assay	[PMID: 27133593]
Bcap37	IC₅₀	22.4 μM Compound: 15	Cytotoxicity against human Bcap37 cells after 48 hrs by MTT assay Cytotoxicity against human Bcap37 cells after 48 hrs by MTT assay	[PMID: 27133593]
Hep 3B2	IC₅₀	22.21 μM Compound: 15	Cytotoxicity against human Hep3B cells after 48 hrs by MTT assay Cytotoxicity against human Hep3B cells after 48 hrs by MTT assay	[PMID: 27133593]
HepG2	IC₅₀	17.01 μM Compound: 15	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 27133593]
MCF7	IC₅₀	>100 μM Compound: 15	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 27133593]
PC-3	IC₅₀	>100 μM Compound: 43	Cytotoxic activity against human PC3 cells assessed as reduction in cell viability after 72 hrs by SRB assay Cytotoxic activity against human PC3 cells assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 28011223]
PC-3	IC₅₀	260 nM Compound: Triptophenolide	Antagonist activity at wild type AR in human PC3 cells assessed as suppression of DHT-induced receptor transcriptional activation after 24 hrs by PSA-luciferase reporter gene assay Antagonist activity at wild type AR in human PC3 cells assessed as suppression of DHT-induced receptor transcriptional activation after 24 hrs by PSA-luciferase reporter gene assay	[PMID: 27994731]
PC-3	IC₅₀	388 nM Compound: Triptophenolide	Antagonist activity at AR T877A mutant (unknown origin) transfected in human PC3 cells assessed as inhibition of DHT-induced receptor transcriptional activation after 24 hrs by PSA-luciferase reporter gene assay Antagonist activity at AR T877A mutant (unknown origin) transfected in human PC3 cells assessed as inhibition of DHT-induced receptor transcriptional activation after 24 hrs by PSA-luciferase reporter gene assay	[PMID: 27994731]
PC-3	IC₅₀	437 nM Compound: Triptophenolide	Antagonist activity at AR W741C/T877A double mutant (unknown origin) transfected in human PC3 cells assessed as inhibition of DHT-induced receptor transcriptional activation after 24 hrs by PSA-luciferase reporter gene assay Antagonist activity at AR W741C/T877A double mutant (unknown origin) transfected in human PC3 cells assessed as inhibition of DHT-induced receptor transcriptional activation after 24 hrs by PSA-luciferase reporter gene assay	[PMID: 27994731]
PC-3	IC₅₀	480 nM Compound: Triptophenolide	Antagonist activity at AR F876L mutant (unknown origin) expressed in human PC3 cells assessed as inhibition of DHT-induced receptor transactivation after 24 hrs by PSA-luciferase reporter gene assay Antagonist activity at AR F876L mutant (unknown origin) expressed in human PC3 cells assessed as inhibition of DHT-induced receptor transactivation after 24 hrs by PSA-luciferase reporter gene assay	[PMID: 27994731]
SK-OV-3	IC₅₀	>100 μM Compound: 43	Cytotoxic activity against human SKOV3 cells assessed as reduction in cell viability after 72 hrs by SRB assay Cytotoxic activity against human SKOV3 cells assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 28011223]
U-251	IC₅₀	>100 μM Compound: 15	Cytotoxicity against human U251 cells after 48 hrs by MTT assay Cytotoxicity against human U251 cells after 48 hrs by MTT assay	[PMID: 27133593]

In Vitro

Triptophenolide (50 nM-5 μM) potently inhibits DHT-induced transcriptional activity of wild-type AR, AR F876L, AR T877A and W741C+T877A AR double mutant in PC-3 cells, with IC₅₀ values of 260 nM, 480 nM, 388 nM and 437 nM, respectively. It shows no agonistic activity toward these AR variants in the absence of DHT^[1].
Triptophenolide (500 nM-5 μM) significantly downregulates prostate-specific antigen mRNA expression in LNCaP cells^[1].
Triptophenolide (0.1-50.0 μM) dose-dependently inhibits the growth of AR-positive LNCaP prostate cancer cells, while having no significant effect on AR-negative PC-3 prostate cancer cell growth^[1].
Triptophenolide (10 nM-10 μM) competitively binds to the androgen receptor ligand-binding domain in a cell-free system with an IC₅₀ of 467 nM^[1].
Triptophenolide (50 nM-5 μM; 24 h) dose-dependently suppresses androgen receptor protein expression in LNCaP cells after 24 hours of treatment, with significant effects at 500 nM and 5 μM^[1].
Triptophenolide (5 μM) efficiently inhibits DHT-induced androgen receptor nuclear translocation in LNCaP cells^[1].
Triptophenolide (0-400 μg/mL; 24/48 h) concentration- and time-dependently inhibits proliferation in MCF‑7 and MDA‑MB‑231 breast cancer cells^[3].
Triptophenolide (180.3 μg/mL for MCF‑7 cells and 322.5 μg/mL for MDA‑MB‑231 cells; 48 h) significantly downregulates target gene mRNA levels as detected and reduces corresponding protein expression as determined in MCF‑7 and MDA‑MB‑231 breast cancer cells^[3].
Triptophenolide (150 μg/mL; 24 h/48 h) induces apoptosis and G1-phase cell cycle arrest, and significantly inhibits migration in MCF-7 and MDA-MB-231 breast cancer cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

LNCaP cells
Concentration:

50 nM, 500 nM, 5 μM
Incubation Time:

24 h
Result:

Effectively suppressed AR protein expression in a dose-dependent manner.
Showed significant suppression at 500 nM and 5 μM.

RT-PCR^[3]

Cell Line:

MCF‑7 and MDA‑MB‑231 breast cancer cells
Concentration:

180.3 μg/mL for MCF‑7 cells and 322.5 μg/mL for MDA‑MB‑231 cells
Incubation Time:

48 h
Result:

significantly upregulates the mRNA expression of multiple pro-apoptotic genes (e.g., BIM, BAK1, BAX, CASP3/9, TP53) and downregulates proliferation-associated genes such as AKT1 in both MCF-7 and MDA-MB-231 breast cancer cells.

Cell Viability Assay^[3]

Cell Line:

MCF‑7 and MDA‑MB‑231 breast cancer cells
Concentration:

0, 100, 200, 300, 400 μg/mL
Incubation Time:

24/48 h
Result:

Inhibits proliferation in MCF‑7 and MDA‑MB‑231 breast cancer cells

Western Blot Analysis^[3]

Cell Line:

MCF‑7 and MDA‑MB‑231 breast cancer cells
Concentration:

180.3 μg/mL for MCF‑7 cells and 322.5 μg/mL for MDA‑MB‑231 cells
Incubation Time:

48 h
Result:

significantly upregulated the expression of pro-apoptotic proteins BIM, BAK1, BAX, and CYCS in both MCF-7 and MDA-MB-231 breast cancer cells.

Cell Cycle Analysis^[3]

Cell Line:

MCF‑7 and MDA‑MB‑231 breast cancer cells
Concentration:

150 μg/mL
Incubation Time:

24 h/48 h
Result:

Induced G1-phase cell cycle arrest in both MCF-7 and MDA-MB-231 breast cancer cells, with a marked increase in G1-phase cell proportion and a corresponding decrease in S-phase cell proportion.

Apoptosis Analysis^[3]

Cell Line:

MCF‑7 and MDA‑MB‑231 breast cancer cells
Concentration:

150 μg/mL
Incubation Time:

24 h/48 h
Result:

Significantly induced apoptosis in both MCF-7 and MDA-MB-231 breast cancer cells, with markedly elevated total apoptosis rates.

Cell Proliferation Assay^[3]

Cell Line:

MCF‑7 and MDA‑MB‑231 breast cancer cells
Concentration:

150 μg/mL
Incubation Time:

24 h/48 h
Result:

Significantly and time-dependently inhibited the migration of both MCF-7 and MDA-MB-231 breast cancer cells, with markedly reduced migration rates at 12 h and 24 h.

In Vivo

Triptophenolide (5-15 mg/kg; intragastric; once daily; 15 days) significantly reduces arthritis scores, suppresses synovial inflammatory factor levels, and alleviates synovial injury in collagen antibody-induced rheumatoid arthritis mice^[2].
Triptophenolide (10 mg/kg; intraperitoneal injection; every 3 days; 21 days) significantly inhibits MCF-7 xenograft tumor growth, reduces tumor weight, and prolongs the survival of tumor-bearing BALB/c nude mice^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/c nude mice (8-10-week-old)^[3]
Dosage:

10 mg/kg
Administration:

intraperitoneal injection; every 3 days; 21 days
Result:

Significantly inhibited MCF-7 xenograft tumor growth, reduced tumor volume and weight, and prolonged the survival of tumor-bearing mice compared to the DMSO control group, with statistically significant improvements.

Animal Model:

BALB/c (8-10-week-old)^[2]
Dosage:

5 mg/kg; 15 mg/kg
Administration:

intragastric; once daily; 15 days
Result:

Significantly reduced mouse arthritis scores compared to the RA group at matching time points.
Suppressed synovial tissue expression of inflammatory factors IL-1β, IL-6, and TNF-α, with levels lower than those in the RA group.
Alleviated synovial injury and reduced inflammatory lesions in joint tissue, with statistically significant improvements compared to the RA group.

Chemical Information

CAS No. 74285-86-2
Appearance Solid
Molecular Weight 312.40
Formula C₂₀H₂₄O₃
Color White to off-white
SMILES

O=C1C(CC[C@]2(C)C3=C(CC[C@]24[H])C(O)=C(C(C)C)C=C3)=C4CO1
Synonyms

Hypolide; (+)-Triptophenolide
Structure Classification
- Terpenoids
- Diterpenoids
- Phenols
- Monophenols
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (320.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.2010 mL

16.0051 mL

32.0102 mL

5 mM

0.6402 mL

3.2010 mL

6.4020 mL

10 mM

0.3201 mL

1.6005 mL

3.2010 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.00 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (287 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. He Y, et al. Identification of Triptophenolide from Tripterygium wilfordii as a Pan-antagonist of Androgen Receptor. ACS Med Chem Lett. 2016 Sep 28;7(12):1024-1027. [Content Brief]

[2]. Pu X, et al. Triptophenolide Improves Rheumatoid Arthritis and Progression by Inducing Macrophage Toxicity. J Biochem Mol Toxicol. 2025;39(1):e70096. [Content Brief]

[3]. Gao J, et al. Triptolide: pharmacological spectrum, biosynthesis, chemical synthesis and derivatives. Theranostics. 2021;11(15):7199-7221. Published 2021 May 24. [Content Brief]

[4]. Sabeel Z, et al. Multi-Targeted Anti-Cancer Effects of Triptophenolide in Hormone-Responsive and Triple-Negative Breast Cancer Models. Int J Mol Sci. 2025 Jun 7;26(12):5469. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.2010 mL	16.0051 mL	32.0102 mL	80.0256 mL
	5 mM	0.6402 mL	3.2010 mL	6.4020 mL	16.0051 mL
	10 mM	0.3201 mL	1.6005 mL	3.2010 mL	8.0026 mL
	15 mM	0.2134 mL	1.0670 mL	2.1340 mL	5.3350 mL
	20 mM	0.1601 mL	0.8003 mL	1.6005 mL	4.0013 mL
	25 mM	0.1280 mL	0.6402 mL	1.2804 mL	3.2010 mL
	30 mM	0.1067 mL	0.5335 mL	1.0670 mL	2.6675 mL
	40 mM	0.0800 mL	0.4001 mL	0.8003 mL	2.0006 mL
	50 mM	0.0640 mL	0.3201 mL	0.6402 mL	1.6005 mL
	60 mM	0.0534 mL	0.2668 mL	0.5335 mL	1.3338 mL
	80 mM	0.0400 mL	0.2001 mL	0.4001 mL	1.0003 mL
	100 mM	0.0320 mL	0.1601 mL	0.3201 mL	0.8003 mL

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Triptophenolide

Bioactive Compound Library Max

Bioactive Compound Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

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Anti-Rheumatic Arthritis Compound Library

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All Caspase Isoforms

All Bcl-2 Family Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Triptophenolide Related Classifications

HY-N0475 Related Classifications