DMU2139
Based on 1 publication(s) in Google Scholar
DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
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- Pureté: 98.0%
- CAS No.: 1821143-80-9
- Formule: C19H15NO2
- Masse moléculaire:289.33
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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
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) DMU2139
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Activité biologique
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CYP1B1 9 nM (IC50) |
CYP1A1 795 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
8.3 μM
Compound: 6j; DMU2139
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Inhibition of human CYP1B1 expressed in HEK293 cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring cisplatin EC50 at 0.018 uM by MTT assay (Rvb = 61 +/- 8 uM)
Inhibition of human CYP1B1 expressed in HEK293 cells assessed as potentiation of cisplatin-induced cytotoxicity by measuring cisplatin EC50 at 0.018 uM by MTT assay (Rvb = 61 +/- 8 uM)
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[PMID: 28222316] |
| HEK293 | IC50 |
0.004 μM
Compound: 6j; DMU2139
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Inhibition of human liver CYP1B1 expressed in HEK293 cells using CEC as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorescence assay
Inhibition of human liver CYP1B1 expressed in HEK293 cells using CEC as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorescence assay
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[PMID: 28222316] |
| HEK293 | IC50 |
0.008 μM
Compound: 6j; DMU2139
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Inhibition of human liver CYP1B1 expressed in HEK293 cells using 7-ethoxyresorufin as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorescence assay
Inhibition of human liver CYP1B1 expressed in HEK293 cells using 7-ethoxyresorufin as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by fluorescence assay
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[PMID: 28222316] |
DMU2139 (6j) shows 88 and 133-fold selectivity for CYP1B1 over CYP1A1 and CYP1A2. In the presence of DMU2139, the EC50 is reversed back to 8.3 μM from 61 μM (seen in CYP1B1-expressing cells without any inhibitor). The EC50 value, in the presence of DMU2139, resembles the EC50 of cisplatin, 8.7μM, in cells transfected with the empty plasmid which has no CYP1B1 gene and therefore cannot express CYP1B1 protein[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1821143-80-9
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Appearance Solid
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Masse moléculaire 289.33
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Formule C19H15NO2
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Color Light yellow to yellow
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SMILES
O=C(C1=CC=C2C=C(OC)C=CC2=C1)/C=C/C3=CC=CN=C3
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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 (1)
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Journal Impact Factor
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Most Recent
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Drug Resist Updat
CYP1B1 promotes PARPi-resistance via histone H1.4 interaction and increased chromatin accessibility in ovarian cancer. [Abstract]2024 Nov:77:101151. PMID: 39395328
Solvant et solubilité
DMSO : 77.5 mg/mL (267.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 5 mg/mL (17.28 mM; Need ultrasonic)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.58 mg/mL (8.92 mM); Clear solution
This protocol yields a clear solution of ≥ 2.58 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.8 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.
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.
Pureté et documentation
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Fiche technique (271 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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Instruction de manipulation (2659 KB)
Références
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 |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 3.4563 mL | 17.2813 mL | 34.5626 mL | 86.4065 mL |
| 5 mM | 0.6913 mL | 3.4563 mL | 6.9125 mL | 17.2813 mL | |
| 10 mM | 0.3456 mL | 1.7281 mL | 3.4563 mL | 8.6407 mL | |
| 15 mM | 0.2304 mL | 1.1521 mL | 2.3042 mL | 5.7604 mL | |
| DMSO | 20 mM | 0.1728 mL | 0.8641 mL | 1.7281 mL | 4.3203 mL |
| 25 mM | 0.1383 mL | 0.6913 mL | 1.3825 mL | 3.4563 mL | |
| 30 mM | 0.1152 mL | 0.5760 mL | 1.1521 mL | 2.8802 mL | |
| 40 mM | 0.0864 mL | 0.4320 mL | 0.8641 mL | 2.1602 mL | |
| 50 mM | 0.0691 mL | 0.3456 mL | 0.6913 mL | 1.7281 mL | |
| 60 mM | 0.0576 mL | 0.2880 mL | 0.5760 mL | 1.4401 mL | |
| 80 mM | 0.0432 mL | 0.2160 mL | 0.4320 mL | 1.0801 mL | |
| 100 mM | 0.0346 mL | 0.1728 mL | 0.3456 mL | 0.8641 mL |
DMU2139 Related Classifications
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