PARP1-IN-5

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PARP1-IN-5 

PARP1-IN-5 是一种低毒、具有口服活性、有效的和有选择性的 PARP-1 抑制剂 (IC50 =14.7 nM)。PARP1-IN-5 可用于癌症研究。

PARP1-IN-5

PARP1-IN-5 Chemical Structure

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PARP1-IN-5 的其他形式现货产品:

PARP1-IN-5 dihydrochloride

生物活性

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

IC50 & Target[1]

PARP-1

14.7 nM (IC50)

PARP-2

0.9 μM (IC50)

体外研究
(In Vitro)

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

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

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

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mice[1]
Dosage: 1000 mg/kg
Administration: P.o.
Result: There was no significant difference in the body weight and blood routine.
Animal Model: Mice[1]
Dosage: 25 and 50 mg/kg
Administration: P.o.; 12 days
Result: Significantly enhanced the inhibitory effect of CBP on A549 cells at 50 mg/kg.
Animal Model: Male Sprague−Dawley (SD) rats[1]
Dosage: 50 mg/kg (Pharmacokinetic Analysis)
Administration: P.o.; 12 days
Result: Positively correlated with the expression of PARP-1.

分子量

464.53

Formula

C25H24N2O5S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Long H, et al. Discovery of Novel Apigenin-Piperazine Hybrids as Potent and Selective Poly (ADP-Ribose) Polymerase-1 (PARP-1) Inhibitors for the Treatment of Cancer. J Med Chem. 2021;64(16):12089-12108.

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