PARP1-IN-5 dihydrochloride 是一种具有口服活性的有效选择性 PARP-1 抑制剂 (IC50 =14.7 nM)。它可用于癌症的研究。

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.

PARP1-IN-5 dihydrochloride (0.1~10 μM) can significantly increase the cytotoxicity of CBP on A549 cells in a dose-dependent manner. PARP1-IN-5 dihydrochloride (0.1~10 μM) decreases the expressions of MCM2-7 on SK-OV-3 cells. PARP1-IN-5 dihydrochloride (0.1~320 μM) has little cytotoxic effects on A549 cells. PARP1-IN-5 dihydrochloride can significantly decrease the PAR level on SK-OV-3 cells[1]. PARP1-IN-5 dihydrochloride exerts antitumor effects through PARP-1. PARP1-IN-5 dihydrochloride could increase the γ-H2AX expression[1].

PARP1-IN-5 dihydrochloride (1000 mg/kg; p.o.) shows that there is no significant difference in the body weight and blood routine[1]. 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[1]. PARP1-IN-5 dihydrochloride (50 mg/kg; p.o.) positively correlates with the expression of PARP-1[1]. PARP1-IN-5 dihydrochloride can decrease the expression of PAR and upregulate the expression of γ-H2AX [1].

T9610

C25H26Cl2N2O5S

537.46

DMSO:125 mg/mL (232.58 mM),Need ultrasonic
H2O:1 mg/mL (1.86 mM),Need ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years