L82
Based on 1 Customer Validation
L82 is a selective and uncompetitive DNA ligase 1 (DNA Lig1) inhibitor (hLig1 IC50=12 μM). L82 shows anti-proliferative activity to breast cancer cells.
For research use only. We do not sell to patients.
- Purity : 98.89%
- CAS No.: 329227-30-7
- Formula: C11H8ClN5O4
- Molecular Weight:309.67
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
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DNA Ligase |
In Vitro
L82 (0-50 μM; 6 d) shows anti-proliferative activity to breast cancer cells[2].
L82 (50 μM; 0-48 h) shows cytostatic activity due to activation of the G1/S checkpoint in MCF7 cells[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:MCF10A, MCF7, HCT116, and HeLa cells
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Concentration:0-50 μM
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Incubation Time:6 days
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Result:Reduced the proliferation of a normal breast epithelial cell line MCF10A and the breast cancer cell lines MCF7, HeLa and HCT116, in a concentration-dependent manner.
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Cell Line:MCF7 cells
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Concentration:50 μM
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Incubation Time:0-48 hours
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Result:Showed a transient accumulation of cells at G2/M after 12 h, then showed an accumulation at G0/G1 that peaked after 24 h.
Decreased in the S phase cell in accompany with the increase in the G0/G1 phase.
Chemical Information
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CAS No. 329227-30-7
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Appearance Solid
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Molecular Weight 309.67
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Formula C11H8ClN5O4
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Color Yellow to orange
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SMILES
O=C1NN=CC(N/N=C/C2=CC=C(C([N+]([O-])=O)=C2)O)=C1Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 33.33 mg/mL (107.63 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)
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Howes TRL, et al. Structure-activity relationships among DNA ligase inhibitors: Characterization of a selective uncompetitive DNA ligase I inhibitor. DNA Repair (Amst). 2017 Dec;60:29-39. [Content Brief]
[2]. Chen X, et al. Rational design of human DNA ligase inhibitors that target cellular DNA replication and repair. Cancer Res. 2008 May 1;68(9):3169-77. [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 |
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| DMSO | 1 mM | 3.2292 mL | 16.1462 mL | 32.2924 mL | 80.7311 mL |
| 5 mM | 0.6458 mL | 3.2292 mL | 6.4585 mL | 16.1462 mL | |
| 10 mM | 0.3229 mL | 1.6146 mL | 3.2292 mL | 8.0731 mL | |
| 15 mM | 0.2153 mL | 1.0764 mL | 2.1528 mL | 5.3821 mL | |
| 20 mM | 0.1615 mL | 0.8073 mL | 1.6146 mL | 4.0366 mL | |
| 25 mM | 0.1292 mL | 0.6458 mL | 1.2917 mL | 3.2292 mL | |
| 30 mM | 0.1076 mL | 0.5382 mL | 1.0764 mL | 2.6910 mL | |
| 40 mM | 0.0807 mL | 0.4037 mL | 0.8073 mL | 2.0183 mL | |
| 50 mM | 0.0646 mL | 0.3229 mL | 0.6458 mL | 1.6146 mL | |
| 60 mM | 0.0538 mL | 0.2691 mL | 0.5382 mL | 1.3455 mL | |
| 80 mM | 0.0404 mL | 0.2018 mL | 0.4037 mL | 1.0091 mL | |
| 100 mM | 0.0323 mL | 0.1615 mL | 0.3229 mL | 0.8073 mL |
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