2. Cell Cycle/DNA Damage Epigenetics Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Apoptosis
  3. PARP DNA/RNA Synthesis Reactive Oxygen Species (ROS) Apoptosis
  4. PARP1-IN-55

PARP1-IN-55 是一种高效且选择性的 PARP1 抑制剂，IC50 值为 0.019 μM。PARP1-IN-55 对 MCF-7 乳腺癌细胞表现出强效的抗增殖选择性活性 (IC50 = 3.6 μM)。PARP1-IN-55 可抑制 PARP1 介导的 DNA 损伤修复通路，诱导 ROS 积累，破坏线粒体膜电位，诱导细胞凋亡 (apoptosis), 并抑制癌细胞的迁移、侵袭和克隆形成。PARP1-IN-55 可用于乳腺癌的研究。

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PARP1-IN-55

PARP1-IN-55 Chemical Structure

CAS No. : 3109617-69-5

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PARP1-IN-55 相关抗体

Top Publications Citing Use of Products

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PARP1-IN-55 is a potent and selective PARP1 inhibitor with an IC50 value of 0.019 μM. PARP1-IN-55 exhibits anti-proliferative selective activity against MCF-7 breast cancer cells (IC50 = 3.6 μM). PARP1-IN-55 inhibits the PARP1-mediated DNA damage repair pathway, induces ROS accumulation, disrupts mitochondrial membrane potential, induced apoptosis and suppresses cancer cell migration, invasion, and colony formation. PARP1-IN-55 can be used for the study of breast cancer[1].

IC50 & Target

PARP1

0.019 μM (IC50)

体外研究
(In Vitro)

PARP1-IN-55 (compound 3f) (48 h) 对 MCF-7 细胞表现出强效的抗增殖活性和高选择性，同时对 L-02 细胞的细胞毒性极小 (IC50 > 100 μM)，选择性指数 (SI) 超过27[1]。
PARP1-IN-55 (1-10 μM；48 h) 以剂量依赖的方式抑制 MCF-7 细胞内 PARP1 的表达[1]。 PARP1-IN-55 (1-10 μM；14 days) 以剂量依赖的方式抑制 MCF-7 细胞的集落形成，10 μM 时可完全抑制集落形成，且对 L-02 细胞几乎无影响[1]。
PARP1-IN-55 (1-10 μM；24 h, 48 h) 以剂量依赖的方式抑制 MCF-7 细胞的迁移和侵袭，10 μM 时可显著下调 MCF-7 细胞中 COL1 蛋白的表达[1]。
PARP1-IN-55 (3-10 μM；48 h) 诱导 MCF-7 细胞发生凋亡，3 μM 时引发早期凋亡，5 μM 和10 μM 时主要引发晚期凋亡，对 L-02 细胞的凋亡诱导作用极小[1]。
PARP1-IN-55 (1-10 μM) 可显著剂量依赖性地增加 MCF-7 细胞内的 ROS 水平，降低线粒体膜电位 (MMP)，破坏细胞膜完整性并诱导大量细胞死亡。它对 L-02 细胞也没有显著影响[1]。
PARP1-IN-55 (1-10 μM；24 h) 升高 MCF-7 细胞中 γH2AX 蛋白的水平，抑制 PARP1 介导的 DNA 损伤修复通路，造成 DNA 损伤的累积[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PARP1-IN-55 相关抗体:

Immunofluorescence[1]

Cell Line: MCF-7 cells
Concentration: 1 μM, 3 μM, 5 μM, 10 μM
Incubation Time: 24 h
Result: Induced a significant concentration-dependent increase in the number of nuclear γH2AX fluorescence foci, indicating accumulation of DNA double-strand breaks.

Cell Invasion Assay[1]

Cell Line: MCF-7 cells
Concentration: 1 μM, 3 μM, 5 μM, 10 μM
Incubation Time: 24 h, 48 h
Result: Inhibits the invasion of MCF-7 cells in a dose-dependent manner, with the inhibitory effect at 10 μM significantly stronger than that of isoalantolactone.

Cell Migration Assay [1]

Cell Line: MCF-7 cells
Concentration: 1 μM, 3 μM, 5 μM, 10 μM
Incubation Time: 24 h, 48 h
Result: Inhibits the migration of MCF-7 cells in a dose-dependent manner.

Cell Proliferation Assay[1]

Cell Line: MCF-7, L-02 cells
Concentration: 1 μM, 3 μM, 5 μM, 10 μM
Incubation Time: 14 days
Result: Inhibits colony formation of MCF-7 cells in a concentration-dependent manner, completely suppressing colony formation at 10 μM; little effect on L-02 cells.

Cell Cytotoxicity Assay[1]

Cell Line: MCF-7, L-02 cells
Concentration: 1 μM, 3 μM, 5 μM, 10 μM
Incubation Time: 24 h
Result: Disrupts the cell membrane integrity of MCF-7 cells, inducing extensive cell death; no effect on the viability of L-02 cells.

Apoptosis Analysis[1]

Cell Line: MCF-7, L-02 cells
Concentration: 3 μM, 5 μM, 10 μM
Incubation Time: 48 h
Result: Induces early apoptosis at 3 μM and mainly late apoptosis at 5 μM/10 μM in MCF-7 cells; minimal apoptotic effect on L-02 cells.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 1 μM, 3 μM, 5 μM, 10 μM
Incubation Time: 48 h
Result: Dose-dependently decreased nuclear PARP1 expression and increased γH2AX expression.
Significantly downregulated COL1 expression at 10 μM.
分子量

429.55

Formula

C25H35NO5
CAS 号
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.
纯度 & 产品资料
参考文献

PARP1-IN-55 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PARP1-IN-553109617-69-5PARPDNA/RNA SynthesisReactive Oxygen Species (ROS)Apoptosispoly ADP ribose polymerase PARP1 inhibitorapoptosiselevate ROSdecrease mitochondrial membrane potentialinhibit migration and invasioninhibit colony formationsuppress DNA damage repairbreast cancerMCF-7 cellsAGS cellsSW620 cellsSU-DHL-10 cellsL-02 cellsInhibitorinhibitorinhibit

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