DMAPT
Based on 2 publication(s) in Google Scholar
DMAPT (Dimethylamino Parthenolide), an analogue of Parthenolide (PTL), is an oral active NF-κB inhibitor, with a LD50 of 1.7 μM for cell population in AML cells. Has potential anti-cancer and anti-metastatic effect.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 98.0%
- CAS No.: 791595-09-0
- Formule: C17H27NO3
- Masse moléculaire:293.40
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) DMAPT
More
Activité biologique
Description
IC50 & Target
NF-κB[1].
In Vitro
DMAPT treatment decreased constitutive NF-κB binding activity, inhibits cell proliferation and viability of PC-3 and DU145 cells[2]. Treatment of PC-3 and DU145 cells with 5 and 4 μM DMAPT, respectively, increases the population doubling times of PC-3 prostate cancer cells from 23.0 ± 5.0 h to 42.0 ± 3.0 h and of the DU145 cells from 20.4 ± 2.2 h to 72.5 ± 24.8 h[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:PC-3 and DU145 cells.
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Concentration:PC-3 cells (0, 2.5, 5 μM), DU145 cells (0 and 4 μM).
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Incubation Time:24 and 48 hours.
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Result:Decreased constitutive NF-κB binding activity, inhibits cell proliferation and viability of PC-3 and DU145 cells.
In Vivo
DMAPT (100 mg/kg, Oral gavage thrice weekly from 42 to 300 days since birth) treatment slows normal tumor development in TRAMP mice, extending the time-to-palpable prostate tumor by 20%[3].
DMAPT further reduces the metastatic area below that of the water vehicle treatment group in lung tissues (0.10% ± 0.15 SD, 92% reduction, p = 0.0028) in TRAMP mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:PC-3 tumor xenograft in athymic nude mice[2].
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Dosage:100 mg/kg.
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Administration:Oral gavage daily for 7 days.
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Result:Increased sensitivity of PC-3 tumor xenografts to X-rays.
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Animal Model:Six-week-old male TRAMP mice[3].
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Dosage:100 mg/kg.
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Administration:Oral gavage thrice weekly from 42 to 300 days since birth.
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Result:Slowed normal tumor development in TRAMP mice, extending the time-to-palpable prostate tumor by 20%.
Chemical Information
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CAS No. 791595-09-0
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Appearance Solid
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Masse moléculaire 293.40
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Formule C17H27NO3
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Color White to off-white
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SMILES
C[C@]12[C@@](O2)([H])[C@]3([H])[C@](CC/C(C)=C\CC1)([H])[C@@H](C(O3)=O)CN(C)C
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Synonyms
Dimethylamino Parthenolide
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Ecotoxicol Environ Saf
Triclosan exposure causes abnormal bile acid metabolism through IL-1β-NF-κB-Fxr signaling pathway. [Abstract]2024 Oct 1:284:116989. PMID: 39260212 -
Commun Biol
NF-κB inhibition attenuates sympathetic hyperreflexia and concomitant development of autonomic dysreflexia and immune dysfunction after spinal cord injury. [Abstract]2025 May 22;8(1):787. PMID: 40404889
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (340.83 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 1.1 mg/mL (3.75 mM; ultrasonic and warming and heat to 40°C)
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (7.09 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (7.09 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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:
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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.
Protocole
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Acute Systemic Toxicity Study
Acute systemic toxicity studies evaluate adverse effects occurring after a single exposure, or repeated exposure within a short acute window, and the main in vivo readouts are mortality, moribund condition, clinical signs, body-weight change, and gross pathological findings; acute oral toxicity methods were developed to replace classical LD50 testing with reduced-animal designs such as fixed-dose procedure, acute toxic class method, and up-and-down procedure. The fixed-dose procedure classifies acute toxicity by administering predefined dose levels and observing evident toxicity rather than using death as the primary endpoint, whereas the acute toxic class method uses sequential groups of three animals per step and the up-and-down procedure doses animals sequentially to estimate an LD50 with fewer animals than conventional LD50 testing.
Pureté et documentation
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Fiche technique (286 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Neelakantan S, et al. Aminoparthenolides as novel anti-leukemic agents: Discovery of the NF-kappaB inhibitor, DMAPT (LC-1). Bioorg Med Chem Lett. 2009 Aug 1;19(15):4346-9. [Content Brief]
[2]. Mendonca MS, et al. DMAPT inhibits NF-κB activity and increases sensitivity of prostate cancer cells to X-rays in vitro and in tumor xenografts in vivo. Free Radic Biol Med. 2017 Nov;112:318-326. [Content Brief]
[3]. Morel KL, et al. Chronic low dose ethanol induces an aggressive metastatic phenotype in TRAMP mice, which is counteracted by parthenolide. Clin Exp Metastasis. 2018 Oct;35(7):649-661. [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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 3.4083 mL | 17.0416 mL | 34.0832 mL | 85.2079 mL |
| DMSO | 5 mM | 0.6817 mL | 3.4083 mL | 6.8166 mL | 17.0416 mL |
| 10 mM | 0.3408 mL | 1.7042 mL | 3.4083 mL | 8.5208 mL | |
| 15 mM | 0.2272 mL | 1.1361 mL | 2.2722 mL | 5.6805 mL | |
| 20 mM | 0.1704 mL | 0.8521 mL | 1.7042 mL | 4.2604 mL | |
| 25 mM | 0.1363 mL | 0.6817 mL | 1.3633 mL | 3.4083 mL | |
| 30 mM | 0.1136 mL | 0.5681 mL | 1.1361 mL | 2.8403 mL | |
| 40 mM | 0.0852 mL | 0.4260 mL | 0.8521 mL | 2.1302 mL | |
| 50 mM | 0.0682 mL | 0.3408 mL | 0.6817 mL | 1.7042 mL | |
| 60 mM | 0.0568 mL | 0.2840 mL | 0.5681 mL | 1.4201 mL | |
| 80 mM | 0.0426 mL | 0.2130 mL | 0.4260 mL | 1.0651 mL | |
| 100 mM | 0.0341 mL | 0.1704 mL | 0.3408 mL | 0.8521 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
DMAPT Related Classifications
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