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-49

PARP1-IN-49 是一种选择性的 PARP1 抑制剂，其 IC50 值为 23.56 nM，Kd 为 17.78 nM。PARP1-IN-49 对 PARP1 的选择性高于 PARP2。PARP1-IN-49 通过抑制 PARP1 导致 DNA 损伤、细胞周期阻滞和凋亡 (apoptosis) 的诱导。PARP1-IN-49 还可增加细胞内活性氧 (ROS) 的水平，并抑制细胞迁移。PARP1-IN-49 可用于乳腺癌和卵巢癌的研究。

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PARP1-IN-49

PARP1-IN-49 Chemical Structure

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PARP1-IN-49 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-49 is a selective PARP1 inhibitor with an IC50 of 23.56 nM and a Kd of 17.78 nM. PARP1-IN-49 shows a selectivity for PARP1 over PARP2. PARP1-IN-49 leads to the induction of DNA damage, cell cycle arrest, and apoptosis. PARP1-IN-49 also increases intracellular ROS levels and inhibits cell migration. PARP1-IN-49 can be used for the research of breast cancer and ovarian cancer[1].

IC50 & Target[1]

PARP1

23.56 nM (IC50)

PARP1

17.78 nM (Kd)

PARP2

285.39 nM (IC50)

体外研究
(In Vitro)

PARP1-IN-49 (compound 9a) (0.5-2 μM; 48 h) 抑制 MDA-MB-231 细胞增殖和迁移[1]。
PARP1-IN-49 (0.5-2 μM; 48 h) 增加了 MDA-MB-231 细胞中与凋亡相关的蛋白质表达，并降低了 Bcl-2 的水平[1]。
PARP1-IN-49 (0.5-2 μM; 48 h) 诱导 MDA-MB-231 细胞中 DNA 损伤和双链断裂[1]。
PARP1-IN-49 (0.5-2 μM；48 小时) 增加 MDA-MB-231 细胞凋亡并导致 S 期细胞周期阻滞[1]。
PARP1-IN-49 (0.5-4 μM；48 小时) 在 MDA-MB-231 细胞中通过诱导 ROS 生成和改变线粒体膜电位诱导细胞凋亡[1]。
PARP1-IN-49 (2 μM；48 小时) 提高 PARP1 的热稳定性，表明直接相互作用[1]。

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

PARP1-IN-49 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5 μM, 1 μM, 2 μM
Incubation Time: 48 h
Result: Inhibited cell proliferation and migration in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5 μM, 1 μM, 2 μM
Incubation Time: 48 h
Result: Induced apoptosis in a dose-dependent manner, increasing the expression of apoptosis-related proteins, such as Cleaved PARP, Cleaved caspase3 and Bax, and decreasing Bcl-2 protein levels.

Immunofluorescence[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5 μM, 1 μM, 2 μM
Incubation Time: 48 h
Result: Induced DNA damage and the accumulation of double-strand breaks, as indicated by increased γH2AX and comet tail length.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5 μM, 1 μM, 2 μM
Incubation Time: 48 h
Result: The proportion of cells in the S phase increased from 20.09% to 47.56%, while the proportion of cells in the G2/M phase decreased from 19.11% to 6.58%.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5 μM, 1 μM, 2 μM
Incubation Time: 48 h
Result: The proportion of cells undergoing early and late apoptosis increased from 0.49% to 53.8%. 
体内研究
(In Vivo)

PARP1-IN-49 (compound 9a) (20, 40 mg/kg；腹腔注射；22 天) 显著抑制 MDA-MB-231 细胞皮下接种到 BALB/c 小鼠体内的肿瘤生长[1]。

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

Animal Model: MDA-MB-231 cells (1 × 107 cells) were subcutaneously inoculated into the right flank of BALB/c nude mice (4-week-old)[1]
Dosage: 20 mg/kg, 40 mg/kg
Administration: Intraperitoneal; 22 days
Result: Tumor growth was significantly inhibited.
分子量

286.26

Formula

C15H11FN2O3
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-49 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

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
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-49PARPDNA/RNA SynthesisReactive Oxygen Species (ROS)Apoptosispoly ADP ribose polymerase PARP1Inhibitorinhibitorinhibit

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