1. Cell Cycle/DNA Damage Epigenetics
  2. PARP
  3. 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。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 PARP1-IN-5 dihydrochloride 通常具有更好的水溶性和稳定性。

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PARP1-IN-5 Chemical Structure

PARP1-IN-5 Chemical Structure

CAS No. : 2735645-53-9

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PARP1-IN-5 的其他形式现货产品:

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

MCE 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].

MCE 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

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-5 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.

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PARP1-IN-5
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HY-132297
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