1. Cell Cycle/DNA Damage Epigenetics
  2. PARP
  3. MC2050

MC2050 是一种选择性 PARP-1 抑制剂,IC50 为 119 nM。MC2050 可在功能上抑制 PARP-1 活性,包括氧化应激诱导的过度激活,并降低 H1 组蛋白的聚 ADP 核糖基化水平。MC2050 可保护神经母细胞瘤细胞免受过氧化氢诱导的氧化应激介导的细胞死亡。MC2050 可用于神经母细胞瘤、伯基特淋巴瘤的相关研究。

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MC2050

MC2050 Chemical Structure

CAS No. : 1301757-19-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MC2050 is a selective PARP-1 inhibitor with an IC50 of 119 nM. MC2050 functionally inhibits PARP-1 activity, including hyperactivation induced by oxidative stress, and reduces the poly (ADP-ribosyl) ation level of histone H1. MC2050 protects neuroblastoma cells from oxidative stress-mediated cell death induced by hydrogen peroxide. MC2050 is applicable to research related to neuroblastoma and Burkitt lymphoma[1].

IC50 & Target[1]

PARP-1

119 nM (IC50)

PARP-2

1.8 μM (IC50)

体外研究
(In Vitro)

MC2050 (25-100 μM; 0-72 h) 不会降低贴壁培养模型中人 SH-SY5Y 神经母细胞瘤细胞的存活率,也不会诱导细胞凋亡[1]
MC2050 (0-100 μM; 0-72 h) 在悬浮培养模型中不会降低 EBV 潜伏感染的人 Raji 伯基特淋巴瘤细胞的存活率[1]
MC2050 (50 μM; 2-24 h) 可在人 SH-SY5Y 神经母细胞瘤细胞中抑制细胞内 PARP-1 活性达 55%-60%,且抑制作用可持续长达 24 h[1]
MC2050 (50 μM; 24-48 h) 在 EBV 潜伏感染和 EBV 诱导裂解的人 Raji 伯基特淋巴瘤细胞中可将细胞内 PARP-1 活性抑制高达 60%[1]
MC2050 (50 μM; 2 h) 可抑制人 SH-SY5Y 神经母细胞瘤细胞中由 H2O2 诱导的 PARP-1 过度激活[1]
MC2050 (50 μM) 可抑制人 SH-SY5Y 神经母细胞瘤细胞中由 H2O2 诱导的 H1 组蛋白多聚 ADP 核糖基化修饰[1]
MC2050 (1-100 μM; 30 min) 可呈浓度依赖性地减轻 H2O2 诱导的人 SH-SY5Y 神经母细胞瘤细胞死亡[1]
MC2050 (50 μM; 24-72 h) 可在 EBV 裂解期诱导的人 Raji 伯基特淋巴瘤细胞中将 EBNA1 蛋白水平提升至最高 2.5 倍[1]

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

Cell Viability Assay[1]

Cell Line: Human SH-SY5Y neuroblastoma cells (adherent culture)
Concentration: 25 μM; 50 μM; 100 μM
Incubation Time: up to 72 h
Result: Did not reduce cell viability compared to untreated controls at concentrations up to 100 μM for up to 72 h.

Western Blot Analysis[1]

Cell Line: EBV-lytic induced human Raji Burkitt lymphoma cells
Concentration: 50 μM
Incubation Time: 24 h, 48 h, 72 h
Result: Increased EBNA1 protein levels in a time-dependent manner, reaching an approximate 2.5-fold increase relative to untreated induced cells after 72 h.
分子量

440.39

Formula

C19H23Cl2N5OS

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
  • 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.

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