Triptophenolide (Synonyms: Hypolide; (+)-Triptophenolide)

Name: Triptophenolide
Brand: MedChemExpress
SKU: HY-N0475
Rating: 4.5 (1 reviews)

Cat. No.: HY-N0475 Purity: 99.98%: Data Sheet
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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.

Triptophenolide Chemical Structure

CAS No. : 74285-86-2

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

Other Forms of Triptophenolide:

Triptophenolide (Standard) Get quote

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Caspase 3

Caspase-9

Bax

Bak

Bim

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	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]
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]
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	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]
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]
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.

Molecular Weight

312.40

Formula

C₂₀H₂₄O₃

CAS No.

74285-86-2

Appearance

Solid

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

Structure Classification

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

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In Vivo:

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

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:

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

Please enter your animal formula composition:

DMSO +

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.98%

Select Batch:

Data Sheet (287 KB) SDS (393 KB)

COA (252 KB) HNMR (109 KB) RP-HPLC (160 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]

Complete Stock Solution Preparation Table

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

Triptophenolide Related Classifications

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Triptophenolide (Synonyms: Hypolide; (+)-Triptophenolide)

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Triptophenolide (Synonyms: Hypolide; (+)-Triptophenolide)

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Triptophenolide Related Antibodies

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Triptophenolide Related Antibodies

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Complete Stock Solution Preparation Table

Triptophenolide Related Classifications

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