| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg |
| Targets |
DMAPT targets NF-κB (nuclear factor kappa-B), acting as an NF-κB inhibitor by alkylating and covalently modifying the reduced cysteine 62 of the p50 subunit, thereby blocking NF-κB activation and downstream signaling pathways involved in inflammation and cancer cell survival.
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| ln Vitro |
In PC-3 and DU145 cells, DMAPT treatment decreased constitutive NF-κB binding activity and impaired cell proliferation and viability [2]. After being treated with 5 and 4 μM DMAPT, the population doubling times of PC-3 and DU145 prostate cancer cells were shown to increase from 23.0 ± 5.0 hours to 42.0 ± 3.0 hours and from 20.4 ± 2.2 hours to 72.5 ± 24.8 hours, respectively[2].
In vitro studies demonstrate that DMAPT inhibits the proliferation and viability of cancer cells, including primary acute myeloid leukemia (AML) cells with an LD50 of 1.7 μM, and reduces constitutive NF-κB binding activity in prostate cancer cell lines such as PC-3 and DU145. |
| ln Vivo |
PC-3 tumor xenografts treated with DMAPT (100 mg/kg, daily oral gavage for 7 days) are more sensitive to X-rays [2]. In TRAMP mice, DMAPT treatment (100 mg/kg, given orally three times a week from days 42 to 300) reduced the rate at which normal tumor development occurred and increased the time it took for palpable prostate tumors by 20% [3]. DMAPT further showed that the lung tissue metastatic area was smaller in TRAMP mice [3] compared to the group treated with water vehicles (0.10% ± 0.15 SD, 92% decrease, p=0.0028).
In vivo, DMAPT suppresses tumor growth in animal models of tobacco-associated neoplasms, including lung and bladder cancer, demonstrating oral bioavailability and anti-tumor efficacy through NF-κB pathway inhibition. |
| Enzyme Assay |
The in vitro NF-κB binding assay involves incubating DMAPT with nuclear extracts from treated cells and an NF-κB consensus oligonucleotide probe, measuring DNA binding activity via electrophoretic mobility shift assay (EMSA) or ELISA-based kits, with inhibition calculated relative to untreated controls.
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| Cell Assay |
In vitro cell culture studies utilize leukemia, prostate cancer, and other cancer cell lines treated with DMAPT at concentrations ranging from 0.1 to 10 μM, assessing cell viability by MTT or trypan blue exclusion, apoptosis via Annexin V/PI staining, and NF-κB target gene expression (e.g., Bcl-2, survivin, cyclin D1) by qPCR or Western blotting.
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| Animal Protocol |
In vivo animal experiments involve oral administration of DMAPT to tumor-bearing mice, monitoring tumor growth inhibition, assessing survival outcomes, performing histopathological analysis of tumors for apoptosis and proliferation markers, and evaluating NF-κB activity in tumor tissues via immunohistochemistry or EMSA.
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| ADME/Pharmacokinetics |
DMAPT is a water-soluble analogue with improved oral bioavailability compared to parthenolide, molecular weight 293.4 g/mol; it is stored as a solid powder at -20°C, with solutions typically prepared in DMSO or aqueous buffers for in vitro and in vivo studies.
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| Toxicity/Toxicokinetics |
Toxicological evaluation of DMAPT shows an LD50 of 1.7 μM against primary AML cells, indicating potent anti-leukemic activity with selectivity for cancer cells; comprehensive animal toxicity studies are limited, though the compound appears to be better tolerated than parthenolide due to improved solubility and bioavailability.
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| References |
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| Additional Infomation |
DMAPT is a research compound not approved for clinical use; it has been investigated as a potential therapeutic agent for hematological malignancies and solid tumors, with ongoing studies exploring its efficacy in combination with other anticancer agents and its mechanism of action as an NF-κB inhibitor.
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| Molecular Formula |
C17H27NO3
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|---|---|
| Molecular Weight |
293.4
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| Exact Mass |
293.199
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| CAS # |
870677-05-7
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| PubChem CID |
129395999
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| Appearance |
White to off-white solid powder
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| LogP |
1.9
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
21
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| Complexity |
459
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C/C/1=C/CC[C@@]2([C@H](O2)[C@@H]3[C@@H](CC1)[C@H](C(=O)O3)CN(C)C)C
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| InChi Key |
UJNSFDHVIBGEJZ-CMRIBGNTSA-N
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| InChi Code |
InChI=1S/C17H27NO3/c1-11-6-5-9-17(2)15(21-17)14-12(8-7-11)13(10-18(3)4)16(19)20-14/h6,12-15H,5,7-10H2,1-4H3/b11-6-/t12-,13+,14-,15+,17+/m0/s1
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| Chemical Name |
(1S,2R,4R,7Z,11S,12S)-12-[(dimethylamino)methyl]-4,8-dimethyl-3,14-dioxatricyclo[9.3.0.02,4]tetradec-7-en-13-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4083 mL | 17.0416 mL | 34.0832 mL | |
| 5 mM | 0.6817 mL | 3.4083 mL | 6.8166 mL | |
| 10 mM | 0.3408 mL | 1.7042 mL | 3.4083 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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