SCR7 pyrazine

SCR7 吡嗪,"6,7-diphenyl-2-sulfanylidene-1H-pteridin-4-one

SCR7 pyrazine is an inhibitor of DNA ligase IV that blocks non-homologous end joining (NHEJ) in a ligase IV‑dependent manner. SCR7 pyrazine enhances the efficiency of Cas9‑mediated homology‑directed repair (HDR). SCR7 pyrazine induces apoptosis and exhibits anticancer activity.

目录号
EY5006
EY5006
EY5006
纯度
99.9%
99.9%
99.9%
规格
1 MG
5 MG
10 MG
原价
360
840
1190
售价
360
840
1190
库存
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    SCR7 is a specific inhibitor of DNA Ligase IV that blocks non-homologous end joining (NHEJ). In mammalian cells and mouse embryos, SCR7 can increase the efficiency of CRISPR/Cas9-mediated, HDR-dependent gene editing by up to 19-fold.

  • 体外研究

    SCR7 effectively inhibits multimer formation at 200 μM and above.

    SCR7 efficiently suppresses cell proliferation in MCF7, A549, HeLa, T47D, A2780, HT1080, and Nalm6 cells, with IC50 values of 40, 34, 44, 8.5, 120, 10, and 50 μM, respectively.
    SCR7 inhibits NHEJ repair of CRISPR-Cas9-induced DSBs.
    In mammalian cells and mouse embryos, SCR7 increases the efficiency of HDR-mediated gene editing using CRISPR/Cas9.

  • 体内研究

  • 激酶实验

    SCR7 inhibits the ligation activity of purified Ligase IV.
    Ligation complementation assays were performed by adding increasing concentrations of purified Ligase IV/XRCC4 complex (30, 60, and 120 fmol), together with oligomeric DNA substrates (5’-compatible and 5’-5’ incompatible ends), to extracts treated with SCR7. Reactions were incubated at 25 °C for 2 h. The reaction products were then resolved on 8% denaturing PAGE. The gel was dried and exposed, and signals were detected by PhosphorImager and analyzed using Multi Gauge (V3.0) software.

  • 细胞实验

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 AKm系数


    例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。


  • 参考文献

    1.An inhibitor of nonhomologous end-joining abrogates double-strand break repair and impedes cancer progression.2012 Dec 21;151(7):1474-87. doi: 10.1016/j.cell.2012.11.054
    2.Small molecules enhance CRISPR/Cas9-mediated homology-directed genome editing in primary cells.Published: 21 August 2017

    分子式
    C18H12N4OS
    分子量
    332.38
    CAS号
    14892-97-8
    储存方式
    -20°C
    溶剂(常温)
    DMSO
    100 mg/mL
    Water
    Ethanol
    Slightly

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。

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