SMER3
Based on 1 Customer Validation
SMER3, a Rapamycin enhancer, is a selective Skp1-Cullin-F-box (SCF)Met30 ubiquitin ligase inhibitor. SMER3 enhances Rapamycin's growth inhibitory effect by inhibition of SCFMet30.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.33%
- No. CAS: 67200-34-4
- Fòrmula: C11H4N4O2
- Peso molecular:224.18
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
1 μM
Compound: 1
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Cytotoxicity against human A549 cells expressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human A549 cells expressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 30508483] |
| A549/TR | IC50 |
0.6 μM
Compound: 1
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Cytotoxicity against human A549/TR cells expressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human A549/TR cells expressing NQO1 assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 30508483] |
| L02 | IC50 |
14.3 μM
Compound: 1
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Cytotoxicity against NQO1 deficient human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against NQO1 deficient human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 30508483] |
| LNCaP C4-2 | IC50 |
0.17 μM
Compound: 7F1; LQZ-7F1
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Cytotoxicity against human LNCaP C4-2 cells assessed as reduction in cell viability incubated for 72 hrs by methylene blue survival assay
Cytotoxicity against human LNCaP C4-2 cells assessed as reduction in cell viability incubated for 72 hrs by methylene blue survival assay
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[PMID: 35504208] |
| LNCaP C4-2 | IC50 |
0.17 μM
Compound: 8; 7F1
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Cytotoxicity against human LNCaP C4-2 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay
Cytotoxicity against human LNCaP C4-2 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay
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[PMID: 38092421] |
| LNCaP C4-2 | IC50 |
0.2 μM
Compound: 7F1; LQZ-7F1
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Cytotoxicity against human LNCaP C4-2 cells with empty vector-transfection assessed as reduction in cell viability incubated for 72 hrs by methylene blue survival assay
Cytotoxicity against human LNCaP C4-2 cells with empty vector-transfection assessed as reduction in cell viability incubated for 72 hrs by methylene blue survival assay
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[PMID: 35504208] |
| LNCaP C4-2 | IC50 |
0.95 μM
Compound: 7F1; LQZ-7F1
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Cytotoxicity against human LNCaP C4-2 cells with survivin overexpression assessed as reduction in cell viability incubated for 72 hrs by methylene blue survival assay
Cytotoxicity against human LNCaP C4-2 cells with survivin overexpression assessed as reduction in cell viability incubated for 72 hrs by methylene blue survival assay
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[PMID: 35504208] |
| PC-3 | IC50 |
0.16 μM
Compound: 7F1; LQZ-7F1
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Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by methylene blue survival assay
Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by methylene blue survival assay
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[PMID: 35504208] |
| PC-3 | IC50 |
0.16 μM
Compound: 8; 7F1
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Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
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[PMID: 38092421] |
In yeast cells, Met4 ubiquitination is blocked in cells exposed to SMER3 (0-60 μM). The met4Δ cells are less susceptible to growth inhibition by SMER3[1].
Addition of SMER3 to the ligase reactions inhibited ubiquitination of Met4 by SCFMet30 in a dose-dependent manner. SMER3 significantly inhibits the binding of Met30 to Skp1, and does not affect the Skp1 and Met30 protein levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 67200-34-4
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Appearance Solid
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Peso molecular 224.18
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Fòrmula C11H4N4O2
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Color Light yellow to green yellow
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SMILES
O=C1C2=NC3=NON=C3N=C2C4=C1C=CC=C4
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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 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 12.5 mg/mL (55.76 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: 1.25 mg/mL (5.58 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
Pureza y Documentación
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Ficha de datos (277 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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.4607 mL | 22.3035 mL | 44.6070 mL | 111.5175 mL |
| 5 mM | 0.8921 mL | 4.4607 mL | 8.9214 mL | 22.3035 mL | |
| 10 mM | 0.4461 mL | 2.2304 mL | 4.4607 mL | 11.1518 mL | |
| 15 mM | 0.2974 mL | 1.4869 mL | 2.9738 mL | 7.4345 mL | |
| 20 mM | 0.2230 mL | 1.1152 mL | 2.2304 mL | 5.5759 mL | |
| 25 mM | 0.1784 mL | 0.8921 mL | 1.7843 mL | 4.4607 mL | |
| 30 mM | 0.1487 mL | 0.7435 mL | 1.4869 mL | 3.7173 mL | |
| 40 mM | 0.1115 mL | 0.5576 mL | 1.1152 mL | 2.7879 mL | |
| 50 mM | 0.0892 mL | 0.4461 mL | 0.8921 mL | 2.2304 mL |
SMER3 Related Classifications
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