Triptophenolide
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.98%
- No. CAS: 74285-86-2
- Fòrmula: C20H24O3
- Peso molecular:312.40
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Chemical Information
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Solvente y solubilidad
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Actividad biológica
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Caspase 3 |
Caspase-9 |
Bax |
Bak |
Bim |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
>60 μM
Compound: Triptophenolide
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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
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[PMID: 38964974] |
| A549 | IC50 |
>100 μM
Compound: 43
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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
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[PMID: 28011223] |
| A549 | IC50 |
42.88 μM
Compound: 15
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Cytotoxicity against human A549 cells after 48 hrs by MTT assay
Cytotoxicity against human A549 cells after 48 hrs by MTT assay
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[PMID: 27133593] |
| Bcap37 | IC50 |
22.4 μM
Compound: 15
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Cytotoxicity against human Bcap37 cells after 48 hrs by MTT assay
Cytotoxicity against human Bcap37 cells after 48 hrs by MTT assay
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[PMID: 27133593] |
| Hep 3B2 | IC50 |
22.21 μM
Compound: 15
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Cytotoxicity against human Hep3B cells after 48 hrs by MTT assay
Cytotoxicity against human Hep3B cells after 48 hrs by MTT assay
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[PMID: 27133593] |
| HepG2 | IC50 |
17.01 μM
Compound: 15
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Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
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[PMID: 27133593] |
| MCF7 | IC50 |
>100 μM
Compound: 15
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Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
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[PMID: 27133593] |
| PC-3 | IC50 |
>100 μM
Compound: 43
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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
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[PMID: 28011223] |
| PC-3 | IC50 |
260 nM
Compound: Triptophenolide
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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
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[PMID: 27994731] |
| PC-3 | IC50 |
388 nM
Compound: Triptophenolide
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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
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[PMID: 27994731] |
| PC-3 | IC50 |
437 nM
Compound: Triptophenolide
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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
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[PMID: 27994731] |
| PC-3 | IC50 |
480 nM
Compound: Triptophenolide
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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
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[PMID: 27994731] |
| SK-OV-3 | IC50 |
>100 μM
Compound: 43
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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
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[PMID: 28011223] |
| U-251 | IC50 |
>100 μM
Compound: 15
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Cytotoxicity against human U251 cells after 48 hrs by MTT assay
Cytotoxicity against human U251 cells after 48 hrs by MTT assay
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[PMID: 27133593] |
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.
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Cell Line:LNCaP cells
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Concentration:50 nM, 500 nM, 5 μM
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Incubation Time:24 h
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Result:Effectively suppressed AR protein expression in a dose-dependent manner.
Showed significant suppression at 500 nM and 5 μM.
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Cell Line:MCF‑7 and MDA‑MB‑231 breast cancer cells
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Concentration:180.3 μg/mL for MCF‑7 cells and 322.5 μg/mL for MDA‑MB‑231 cells
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Incubation Time:48 h
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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.
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Cell Line:MCF‑7 and MDA‑MB‑231 breast cancer cells
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Concentration:0, 100, 200, 300, 400 μg/mL
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Incubation Time:24/48 h
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Result:Inhibits proliferation in MCF‑7 and MDA‑MB‑231 breast cancer cells
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Cell Line:MCF‑7 and MDA‑MB‑231 breast cancer cells
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Concentration:180.3 μg/mL for MCF‑7 cells and 322.5 μg/mL for MDA‑MB‑231 cells
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Incubation Time:48 h
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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.
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Cell Line:MCF‑7 and MDA‑MB‑231 breast cancer cells
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Concentration:150 μg/mL
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Incubation Time:24 h/48 h
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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.
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Cell Line:MCF‑7 and MDA‑MB‑231 breast cancer cells
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Concentration:150 μg/mL
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Incubation Time:24 h/48 h
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Result:Significantly induced apoptosis in both MCF-7 and MDA-MB-231 breast cancer cells, with markedly elevated total apoptosis rates.
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Cell Line:MCF‑7 and MDA‑MB‑231 breast cancer cells
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Concentration:150 μg/mL
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Incubation Time:24 h/48 h
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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.
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.
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Animal Model:BALB/c nude mice (8-10-week-old)[3]
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Dosage:10 mg/kg
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Administration:intraperitoneal injection; every 3 days; 21 days
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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.
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Animal Model:BALB/c (8-10-week-old)[2]
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Dosage:5 mg/kg; 15 mg/kg
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Administration:intragastric; once daily; 15 days
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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
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No. CAS 74285-86-2
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Appearance Solid
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Peso molecular 312.40
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Fòrmula C20H24O3
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Color White to off-white
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SMILES
O=C1C(CC[C@]2(C)C3=C(CC[C@]24[H])C(O)=C(C(C)C)C=C3)=C4CO1
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Synonyms
Hypolide; (+)-Triptophenolide
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Structure Classification
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Initial Source
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (287 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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
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.
| 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
HY-N0475 Related Classifications
Powered by Bioz
- Triptophenolide
- 74285-86-2
- Hypolide
- (+)-Triptophenolide
- Androgen Receptor
- Pyroptosis
- Caspase
- Bcl-2 Family
- Apoptosis
- prostate-specific antigen
- F876L mutant androgen receptor
- W741C+T877A double mutant androgen receptor
- androgen receptor
- human wild-type AR
- PC-3 cells
- T877A mutant androgen receptor
- rheumatoid arthritis
- AR-positive prostate cancer cells
- LNCaP cells
- Inhibitor
- inhibitor
- inhibit