LEM-14
Based on 1 Customer Validation
LEM-14 is a potent and selective NSD2 inhibitor with an IC50 of 132 µM. LEM-14 has very weak activitv against NSD1 and has no activity against NSD3. LEM-14 inhibits fibrotic gene expression in ND but not DIO BMDMs. LEM-14 combined with ionizing radiation (IR) enhances the apoptosis rate and reduces the colony-formation ability of CRC cells. LEM-14 exhibits enhanced anti-tumor efficacy in Balb/c nude mice bearing LoVo cell xenografts when combined with ionizing radiation. LEM-14 has the potential for the research of multiple myeloma and colorectal cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.02%
- No. CAS: 1814881-70-3
- Fòrmula: C25H26N4O4S
- Peso molecular:478.56
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Almacenamiento:Powder -20°C, 3 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
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Apoptosis Compound Library
HY-L003
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Epigenetics Compound Library
HY-L005
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Histone Modification Research Compound Library
HY-L024
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Anti-Cancer Compound Library
HY-L025
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Covalent Screening Library
HY-L036
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Reprogramming Compound Library
HY-L039
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Anti-Blood Cancer Compound Library
HY-L079
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Anti-Colorectal Cancer Compound Library
HY-L103
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Heterocyclic Compound Library
HY-L138
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Highly Selective Inhibitors Library
HY-L158
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Highly Selective Activators Library
HY-L159
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Cell Death Library
HY-L162
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Anti-Hematopathy Compound Library
HY-L171
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Covalent Screening Library Plus
HY-L036P
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Bioactive Compound Library
HY-L001
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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Methylation Compound Library
HY-L203
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High-Throughput Bioactive Compound Library
HY-L205
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Posttranslational Modification Library
HY-L226
Ver todos los productos específicos de isoformas Histone Methyltransferase
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Actividad biológica
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NSD2 132 μM (IC50) |
LEM-14 (15-30 μM, 48 h) combined with ionizing radiation (IR) to treat colorectal cancer (CRC) cells, enhances the apoptosis rate and reduces the colony-formation ability of CRC cells (HCT116 and LoVo)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 and LoVo cells
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Concentration:30 μM
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Incubation Time:48 h
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Result:Enhanced the apoptosis rate of CRC cells combined with ionizing radiation (IR).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LoVo cells (2 × 106) were subcutaneously implanted into the flanks of 6-8-week-old Balb/c nude mice[1]
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Dosage:5 mg/kg
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Administration:i.p., 2 consecutive days injection + 2 days interval, 28 days
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Result:Achieved tumor growth inhibition.
Showed no significant changes in body weight.
Reduced the Ki67 expression.
Chemical Information
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No. CAS 1814881-70-3
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Appearance Solid
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Peso molecular 478.56
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Fòrmula C25H26N4O4S
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Color Light brown to gray
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SMILES
O=C1C(C2=C(CCCC2)S3)=C3NC(CN4CCN(C([C@H]5CC6=CC=CC=C6C(O5)=O)=O)CC4)=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 50 mg/mL (104.48 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.
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 (276 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]. Shen Y, et al. Identification of LEM-14 inhibitor of the oncoprotein NSD2. Biochem Biophys Res Commun. 2019 Jan 1;508(1):102-108. [Content Brief]
[3]. Li X, et al. NSD2 methylates AROS to promote SIRT1 activation and regulates fatty acid metabolism-mediated cancer radiotherapy. Cell Rep. 2023 Oct 31;42(10):113126. [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, 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 | 2.0896 mL | 10.4480 mL | 20.8960 mL | 52.2401 mL |
| 5 mM | 0.4179 mL | 2.0896 mL | 4.1792 mL | 10.4480 mL | |
| 10 mM | 0.2090 mL | 1.0448 mL | 2.0896 mL | 5.2240 mL | |
| 15 mM | 0.1393 mL | 0.6965 mL | 1.3931 mL | 3.4827 mL | |
| 20 mM | 0.1045 mL | 0.5224 mL | 1.0448 mL | 2.6120 mL | |
| 25 mM | 0.0836 mL | 0.4179 mL | 0.8358 mL | 2.0896 mL | |
| 30 mM | 0.0697 mL | 0.3483 mL | 0.6965 mL | 1.7413 mL | |
| 40 mM | 0.0522 mL | 0.2612 mL | 0.5224 mL | 1.3060 mL | |
| 50 mM | 0.0418 mL | 0.2090 mL | 0.4179 mL | 1.0448 mL | |
| 60 mM | 0.0348 mL | 0.1741 mL | 0.3483 mL | 0.8707 mL | |
| 80 mM | 0.0261 mL | 0.1306 mL | 0.2612 mL | 0.6530 mL | |
| 100 mM | 0.0209 mL | 0.1045 mL | 0.2090 mL | 0.5224 mL |
LEM-14 Related Classifications
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