2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. PARP DNA/RNA Synthesis Apoptosis CDK Bcl-2 Family
  4. PARP1-IN-50

PARP1-IN-50 是一种选择性且有口服活性的 PARP-1 抑制剂，其 IC50 为 64.98 nM。PARP1-IN-50 能够抑制 PAR 的形成并诱导 DNA 双链断裂，从而造成 DNA 损伤。PARP1-IN-50 可以诱导 G2/M 期阻滞和癌细胞凋亡 (apoptosis)。PARP1-IN-50 对多种癌细胞表现出显著的抗增殖活性。PARP1-IN-50 可用于癌症的研究，如乳腺癌 。

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PARP1-IN-50

PARP1-IN-50 Chemical Structure

CAS No. : 2255341-36-5

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PARP1-IN-50 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

查看 CDK 亚型特异性产品:

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

查看 Bcl-2 Family 亚型特异性产品:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PARP1-IN-50 is a selective and orally active PARP-1 inhibitor with an IC50 of 64.98 nM. PARP1-IN-50 can inhibit PAR formation and induce DNA double strand breaks, thereby causing DNA damage. PARP1-IN-50 can induce G2/M phase arrest and cancer cells apoptosis. PARP1-IN-50 demonstrates significant antiproliferative activity against various cancer cells. PARP1-IN-50 can be used for the research of cancer, such as breast cancer[1].

IC50 & Target[1]

PARP-1

64.98 nM (IC50)

Cdk1/cyclin B

 

Bcl-2

 

Bax

 

体外研究
(In Vitro)

PARP1-IN-50 (Compound 13) 在 HCC-1937、Capan-1、MCF-7 和 PANC-1 细胞中表现出显著的抗增殖活性，其 IC50 值分别为 0.88，0.56，4.49 和 1.53 μM[1]。
PARP1-IN-50 (1-10 μM, 48 h) 在 HCC-1937 细胞中会诱导 G2/M 期阻滞，并抑制 CDK1 和细胞周期蛋白 B 的表达水平[1]。
PARP1-IN-50 (1-10 μM, 4 h) 抑制HCC-1937 细胞中HCC-1937 细胞中 H2O2诱导的 PAR 的形成[1]。
PARP1-IN-50 (1-10 μM, 30 mins) 增加了 HCC-1937 细胞中 PARP-1-DNA 的捕获，并诱导 DNA 双链断裂[1]。
PARP1-IN-50 (1-10 μM, 48 h) 诱导 HCC-1937 细胞凋亡[1]。

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

PARP1-IN-50 相关抗体:

Cell Proliferation Assay[1]

Cell Line: HCC-1937, Capan-1, MCF-7, PANC-1, A549, H460, CaCo-2, HL-7702
Concentration: 20 μM
Incubation Time: 48 h
Result: Showed an inhibition rate of 100% in SK-OV-3 cells, 84.36% in PANC-1, 44.68% in H460 cells, 75.89 % in HL-7702 cells and 68.33% in MCF-7 cells.

Western Blot Analysis[1]

Cell Line: HCC-1937 cells
Concentration: 1, 5 and 10 μM
Incubation Time: 0.5, 4 and 48 h
Result: Inhibited PAR levels and increased the PARP-1-DNA trapping levles.
Increased γ-H2AX protein levels.
Reduced CDK1 and cyclin B levles.
Upregulated the expression of Bax and downregulated the expression of Bcl-2.
体内研究
(In Vivo)

PARP1-IN-50 (Compound 13) (25-50 mg/kg，口服，每天一次，持续 21 天) 在 BALB/c 裸鼠中显著抑制 HCC-1937 异种移植肿瘤的生长，且具有良好的安全性特征[1]。

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

Animal Model: BALB/c nude mice with HCC-1937 xenograft (female, 5-6 weeks, 18-22 g )[1]
Dosage: 25 mg/kg, 50 mg/kg
Administration: Orally administration
Result: Showed growth inhibition rates of 53.5% and 71.4% at 25 mg/kg and 50 mg/kg.
Reduced tumor weight and volume.
Had no significant changes in body weight and no significant organ toxicity.
Reduced Ki67 expression and increased γ-H2AX expression.
分子量

662.42

Formula

C22H26Br2N6O4S2
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-50 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

PARP1-IN-502255341-36-5PARPDNA/RNA SynthesisApoptosisCDKBcl-2 Familypoly ADP ribose polymerase Cyclin dependent kinaseHCC-1937Capan-1MCF-7PANC-1A549H460CaCo-2HL-7702γ-H2AXBaxbcl-2CDK1cyclin BInhibitorinhibitorinhibit

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