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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 | Availability | 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) | $259 | 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 | PARP2:0.9 μM, PARP1:14.7 nM |
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. | ||||||||||||||||||||||||||||||||||||||||
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. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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