PARP-1-IN-3
Based on 1 Customer Validation
PARP-1-IN-3, a benzamide derivative, is a potent PARP-1 inhibitor with IC50 values of 0.25 nM and 2.34 nM for PARP-1 and PARP-2, respectively. PARP-1-IN-3 induces apoptosis and arrest cell cycle at G2/M phase. PARP-1-IN-3 can be used in research of cancer.
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- Purity : 99.80%
- CAS No.: 2976342-33-1
- 화학식: C21H17BrN2O3
- 분자량:425.28
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보관: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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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
IC50 & Target
[1]|
PARP-1 0.25 nM (IC50) |
PARP-2 2.34 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DLD-1 | IC50 |
2.83 μM
Compound: 13f
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Antiproliferative activity against human DLD-1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human DLD-1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 36921527] |
| HCT-116 | IC50 |
0.3 μM
Compound: 13f
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Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 36921527] |
| NCM460 | IC50 |
486.87 μM
Compound: 13f
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Cytotoxicity against human NCM460 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against human NCM460 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 36921527] |
| SW480 | IC50 |
33.69 μM
Compound: 13f
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Antiproliferative activity against human SW480 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human SW480 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 36921527] |
In Vitro
PARP-1-IN-3 (compound 13f; 48 h) has potent anticancer activity with IC50 values of 0.30, 2.83, 33.69, and 486.87 μM for HCT116, DLD-1, SW480, and NCM460 cells, respectively[1].
PARP-1-IN-3 (0.3-3 μM; 24-48 h) inhibits colony formation and migration of HCT116 cells[1].
PARP-1-IN-3 (0.3-3 μM; 48 h) induces accumulation of DNA double-strand breaks in HCT116 cells[1].
PARP-1-IN-3 (0.3-7.5 μM; 48-72 h) arrests cell cycle at G2/M phase, reduces mitochondrial membrane potential and ultimately induce apoptosis in HCT116 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 cells
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Concentration:0.3, 1.5, 7.5 μM
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Incubation Time:48 and 72 h
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Result:Increased the percentage of total apoptotic cells from 1.05% (control group) to 79.49% (7.5 μM).
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Cell Line:HCT116 cells
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Concentration:0.3, 1.5, 7.5 μM
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Incubation Time:48 and 72 h
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Result:Blocked the cell cycle progression at G2/M phase.
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Cell Line:HCT116 cells
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Concentration:0.3, 1, 3 μM
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Incubation Time:48 h
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Result:Increased expression levels of γH2AX in a concentration-dependent manner.
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Cell Line:HCT116 cells
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Concentration:0.3, 1, 3 μM
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Incubation Time:48 h
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Result:Increased the expression levels of Bax, cleaved Caspase-3 and cleaved-PARP, and decreased the expression level of Bcl-2.
Chemical Information
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CAS No. 2976342-33-1
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Appearance Solid
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분자량 425.28
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화학식 C21H17BrN2O3
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Color White to light yellow
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SMILES
NC(C1=CC=CC=C1OCC2=CC=CC(NC(C3=CC=C(C=C3)Br)=O)=C2)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 125 mg/mL (293.92 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)
순도&문서
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 | 2.3514 mL | 11.7570 mL | 23.5139 mL | 58.7848 mL |
| 5 mM | 0.4703 mL | 2.3514 mL | 4.7028 mL | 11.7570 mL | |
| 10 mM | 0.2351 mL | 1.1757 mL | 2.3514 mL | 5.8785 mL | |
| 15 mM | 0.1568 mL | 0.7838 mL | 1.5676 mL | 3.9190 mL | |
| 20 mM | 0.1176 mL | 0.5878 mL | 1.1757 mL | 2.9392 mL | |
| 25 mM | 0.0941 mL | 0.4703 mL | 0.9406 mL | 2.3514 mL | |
| 30 mM | 0.0784 mL | 0.3919 mL | 0.7838 mL | 1.9595 mL | |
| 40 mM | 0.0588 mL | 0.2939 mL | 0.5878 mL | 1.4696 mL | |
| 50 mM | 0.0470 mL | 0.2351 mL | 0.4703 mL | 1.1757 mL | |
| 60 mM | 0.0392 mL | 0.1959 mL | 0.3919 mL | 0.9797 mL | |
| 80 mM | 0.0294 mL | 0.1470 mL | 0.2939 mL | 0.7348 mL | |
| 100 mM | 0.0235 mL | 0.1176 mL | 0.2351 mL | 0.5878 mL |
PARP-1-IN-3 Related Classifications
HY-149800 Related Classifications
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