PARP-1-IN-1

发表于由

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。

PARP-1-IN-1 

PARP-1-IN-1 是一种高选择性且具有口服活性的 PARP-1 抑制剂 (IC50=0.96 nM)。PARP-1-IN-1 在 MDA-MB-436 异种移植模型中具有良好的耐受性和显著的单剂量活性。

PARP-1-IN-1

PARP-1-IN-1 Chemical Structure

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生物活性

PARP-1-IN-1 is a high selective and orally active PARP-1 inhibitor (IC50=0.96 nM). PARP-1-IN-1 has well tolerance and remarkable single dose activity in the MDA-MB-436 xenotransplantation model[1].

体外研究
(In Vitro)

PARP-1-IN-1 (compound Y49) (48 hours) has effective inhibition on different cancer cells (IC50s of 9.64, 123.5 106.3 μM for MX-1, MCF7 and A548 cells, respectively)[1].
PARP-1-IN-1 (2.5-10 μM, 48 hours) successfully inhibits the activity of PARP-1 and reduces the production of PAR in A549 cells, which is dose-dependent to some extent[1].

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

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 2.5 μM, 5 μM and 10 μM
Incubation Time: 48h
Result: Inhibited the activity of PARP-1 successfully and reduced the production of PAR in cancer cells. PARP-1-IN-1 was dose-dependent to some extent.

体内研究
(In Vivo)

PARP-1-IN-1 (compound Y49) (50 mg/kg/day; p.o.; daily for 18 days) inhibits the growth of MDA-MB-436 tumor in BALB/c nude mice[1].

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

Animal Model: Female athymic BALB/c nude mice (inoculated MDA-MB-436 cells)[1]
Dosage: 50 mg/kg
Administration: p.o., daily for 18 days
Result: Inhibited the growth of MDA-MB-436 tumor significantly, and no significant change in the body weight of PARP-1-IN-1 treated mice.

分子量

392.47

Formula

C23H25FN4O
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]. Yu J, et al. Structure-based design, synthesis, and evaluation of inhibitors with high selectivity for PARP-1 over PARP-2. Eur J Med Chem. 2022;227:113898.

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