PARP1-IN-5 dihydrochloride 

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。

CAS号

2823308-89-8

分子式

C25H26Cl2N2O5S

主要靶点

PARP

仅限科研使用

Cat No : CM10126

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Synonyms



产品信息

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.

CAS号 2823308-89-8
分子式 C25H26Cl2N2O5S
主要靶点 PARP
主要通路 表观遗传|DNA损伤和修复
分子量 537.46
纯度 96.03%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

PARP-2:0.9 μM|PARP-1:14.7 nM

体内活性

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].

体外活性

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].

溶解度

H2O:1 mg/mL (1.86 mM),Need ultrasonic and warming and heat to 60°C,DMSO:125 mg/mL (232.58 mM),Sonification is recommended.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
×
=
×
C1   V1   C2   V2