1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. PARP Apoptosis
  3. PARP1-IN-12

PARP1-IN-12 是一种有效的 PARP1 抑制剂,其 IC50 值为 2.99 nM。PARP1-IN-12 具有较好的抗癌细胞增殖活性,可诱导细胞凋亡并使细胞周期停滞在 G2/M 期。PARP1-IN-12 能在 BRCA 缺陷的细胞中诱导 DNA 双链断裂 (DSBs)。

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PARP1-IN-12 Chemical Structure

PARP1-IN-12 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PARP1-IN-12 is a potent PARP1 inhibitor with an IC50 of 2.99 nM. PARP1-IN-12 exhibits antiproliferative activity, can induce cell apoptosis and cause cycle arrest at G2/M phase. PARP1-IN-12 also can induce DNA double strand breaks (DSBs) in BRCA-deficient cells[1].

IC50 & Target

PARP-1

2.99 nM (IC50)

体外研究
(In Vitro)

PARP1-IN-12 (compound 20e) (0.1, 0.3, 1 µM; 48 h) exhibits activities of antiproliferation and selectively killing BRCA-deficient cells, can also induce DNA double strand breaks (DSBs) in BRCA-deficient cells in a concentration-dependent manner[1].
PARP1-IN-12 (10 µM, 48 h) enhances the protein levels of phosphorylated Chk1[1].
PARP1-IN-12 (1, 3, 10 µM; 48 h) activats cell cycle checkpoints, then induces G2/M arrest in BRCA-deficient cells and (1, 5, 10 µM; 96 h) also induces MDA-MB-436 cells apoptosis in a concentration-dependent manner[1].

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

Cell Proliferation Assay[1]

Cell Line: UWB1.289 (BRCA1-deficient), UWB1.289+BRCA1 (BRCA1 restored), MDA-MB-436 (BRCA1-deficient), Capan-1 (BRCA2-deficient) cells
Concentration: 0.1, 0.3, 1 µM
Incubation Time: 48 h
Result: Showed antiproliferative activity with IC50s of 0.27, 1.43, 0.87, 0.19 µM for UWB1.289, UWB1.289+BRCA1, Capan-1 and MDA-MB-436 cells, respectively.

Immunofluorescence[1]

Cell Line: MDA-MB-436, Capan-1 cells
Concentration: 10 µM
Incubation Time: 48 h
Result: Enhanced the protein levels of phosphorylated Chk1 but the levels of corresponding total proteins were not altered.

Cell Cycle Analysis[1]

Cell Line: Capan-1 cells
Concentration: 1, 3, 10 µM
Incubation Time: 48 h
Result: Induced G2/M arrest in BRCA-deficient cells in a concentration-dependent manner.

Apoptosis Analysis[1]

Cell Line: MDA-MB-436 cells
Concentration: 1, 5, 10 µM
Incubation Time: 96 h
Result: Caused apoptosis in a concentration-dependent manner in MDA-MB-436 cells.

Western Blot Analysis[1]

Cell Line: MDA-MB-436, Capan-1 cells
Concentration: 0.1, 0.3, 1 µM
Incubation Time: 48 h
Result: Induced increased levels of γH2AX in a concentration-dependent manner in both MDA-MB-436 and Capan-1 cells.
分子量

741.93

Formula

C43H56FN5O5

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
  • 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 *
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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
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.

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产品名称:
PARP1-IN-12
目录号:
HY-150765
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