PARP1-IN-49
PARP1-IN-49 is a selective PARP1 inhibitor with an IC50 of 23.56 nM and a Kd of 17.78 nM. PARP1-IN-49 shows a selectivity for PARP1 over PARP2. PARP1-IN-49 leads to the induction of DNA damage, cell cycle arrest, and apoptosis. PARP1-IN-49 also increases intracellular ROS levels and inhibits cell migration. PARP1-IN-49 can be used for the research of breast cancer and ovarian cancer.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C15H11FN2O3
- Masse moléculaire:286.26
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Voir tous les produits spécifiques à Isoform DNA/RNA Synthesis
More
Activité biologique
|
PARP1 23.56 nM (IC50) |
PARP1 17.78 nM (Kd) |
PARP2 285.39 nM (IC50) |
PARP1-IN-49 (compound 9a) (0.5-2 μM; 48 h) inhibits MDA-MB-231 cell proliferation and migration[1].
PARP1-IN-49 (0.5-2 μM; 48 h) increases apoptosis-related protein expression and decreases Bcl-2 levels in MDA-MB-231 cells[1].
PARP1-IN-49 (0.5-2 μM; 48 h) induces DNA damage and double-strand breaks MDA-MB-231 cells[1].
PARP1-IN-49 (0.5-2 μM; 48 h) increases apoptosis and causes S phase cell cycle arrest MDA-MB-231 cells[1].
PARP1-IN-49 (0.5-4 μM; 48 h) induces apoptosis via ROS generation and altered mitochondrial membrane potential MDA-MB-231 cells[1].
PARP1-IN-49 (2 μM; 48 h) enhances PARP1 thermal stability, indicating direct interaction[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MDA-MB-231 cells
-
Concentration:0.5 μM, 1 μM, 2 μM
-
Incubation Time:48 h
-
Result:Inhibited cell proliferation and migration in a dose-dependent manner.
-
Cell Line:MDA-MB-231 cells
-
Concentration:0.5 μM, 1 μM, 2 μM
-
Incubation Time:48 h
-
Result:Induced apoptosis in a dose-dependent manner, increasing the expression of apoptosis-related proteins, such as Cleaved PARP, Cleaved caspase3 and Bax, and decreasing Bcl-2 protein levels.
-
Cell Line:MDA-MB-231 cells
-
Concentration:0.5 μM, 1 μM, 2 μM
-
Incubation Time:48 h
-
Result:Induced DNA damage and the accumulation of double-strand breaks, as indicated by increased γH2AX and comet tail length.
-
Cell Line:MDA-MB-231 cells
-
Concentration:0.5 μM, 1 μM, 2 μM
-
Incubation Time:48 h
-
Result:The proportion of cells in the S phase increased from 20.09% to 47.56%, while the proportion of cells in the G2/M phase decreased from 19.11% to 6.58%.
-
Cell Line:MDA-MB-231 cells
-
Concentration:0.5 μM, 1 μM, 2 μM
-
Incubation Time:48 h
-
Result:The proportion of cells undergoing early and late apoptosis increased from 0.49% to 53.8%.
| Species | Dose | Route | Note | Tmax | Cmax | AUC0-t | T1/2 | MRT |
|---|---|---|---|---|---|---|---|---|
| Rat[1] | 5 mg/kg | i.p. | 文献审核 | 0.39 h | 6993.33 ng/mL | 11115.57 ng·h/mL | 1.5 h | 1.13 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:MDA-MB-231 cells (1 × 107 cells) were subcutaneously inoculated into the right flank of BALB/c nude mice (4-week-old)[1]
-
Dosage:20 mg/kg, 40 mg/kg
-
Administration:Intraperitoneal; 22 days
-
Result:Tumor growth was significantly inhibited.
Chemical Information
-
Masse moléculaire 286.26
-
Formule C15H11FN2O3
-
SMILES
O=C(NC)C1=CC(C2=CC=C(OC(N3)=O)C3=C2)=CC(F)=C1
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PARP1-IN-49 Related Classifications
HY-179406 Related Classifications
Powered by Bioz