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PARP1-IN-5 dihydrochloride is an orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $84 | - | In Stock | |
| 5 mg | $198 | - | In Stock | |
| 10 mg | $313 | - | In Stock | |
| 25 mg | $622 | - | In Stock | |
| 50 mg | $872 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $243 | - | In Stock |
| Description | PARP1-IN-5 dihydrochloride is an orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer. |
| Targets&IC50 | PARP1:14.7 nM, PARP2:0.9 μM |
| In vitro | PARP1-IN-5 dihydrochloride (0.1~320 μM) significantly enhances CBP cytotoxicity on A549 cells in a dose-dependent manner but has minimal cytotoxic effects on A549 cells alone. It also decreases MCM2-7 expression and PAR levels in SK-OV-3 cells and increases γ-H2AX expression, exhibiting antitumor effects via PARP-1[1]. |
| In vivo | PARP1-IN-5 dihydrochloride (1000 mg/kg; p.o.) shows no significant difference in body weight and blood routine. PARP1-IN-5 dihydrochloride (25 and 50 mg/kg; p.o.; 12 days) significantly enhances the inhibitory effect of carboplatin on A549 cells at 50 mg/kg. PARP1-IN-5 dihydrochloride (50 mg/kg; p.o.) positively correlates with the expression of PARP-1. PARP1-IN-5 dihydrochloride decreases the expression of PAR and upregulates the expression of γ-H2AX [1]. |
| Molecular Weight | 537.46 |
| Formula | C25H26Cl2N2O5S |
| Cas No. | 2823308-89-8 |
| Smiles | O=C1C=C(C2=CC=C(O)C=C2)OC3=C(CN4CCN(CC5=CC=CS5)CC4)C(O)=CC(O)=C31.Cl[H].Cl[H] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 125 mg/mL (232.58 mM), Sonication is recommended. H2O: 1 mg/mL (1.86 mM), Sonication and heating to 60℃ are recommended. | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (7.44 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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