| Bioactivity | SCR7 is an unstable form that can be autocyclized into a stable form SCR7 pyrazine (HY-107845). SCR7 pyrazine is a DNA ligase IV inhibitor that blocks nonhomologous end-joining (NHEJ) in a ligase IV-dependent manner. SCR7 pyrazine is also a CRISPR/Cas9 enhancer which increases the efficiency of Cas9-mediated homology-directed repair (HDR). SCR7 pyrazine induces cell apoptosis and has anticancer activity[1][2]. | ||||||||||||
| Invitro | SCR7 (SCR7 pyrazine；20-100 μM；24 小时；MCF7 细胞) 处理会干扰细胞中的 NHEJ，导致未修复的双链断裂 (DSB) 累积[1]。 SCR7 (SCR7 pyrazine) 处理显示细胞增殖呈剂量依赖性降低，MCF7 的 IC50 值为 40 μM、34 μM、44 μM、8.5 μM、120 μM、10 μM 和 50 μM，A549、HeLa、T47D、A2780、HT1080 和 Nalm6 细胞[1]。在 MCF7 细胞中，SCR7 (SCR7 pyrazine；20、40 μM) 处理增加 ATM 的磷酸化并激活p53，减少 MDM2、BCL2，导致促凋亡蛋白、PUMA 和 BAX 的激活。并且 MCL1、PARP1、Caspase 3 和 Caspase 9 切割的较短片段以剂量依赖的方式上调[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> SCR7 相关抗体: Western Blot Analysis[1] Cell Line: | ||||||||||||
| In Vivo | SCR7 (SCR7 pyrazine；10 mg/kg；腹腔注射；六次剂量；BALB/c 小鼠) 处理显著减少了乳腺癌引起的肿瘤并延长了寿命[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: | ||||||||||||
| CAS | 1533426-72-0 | ||||||||||||
| Formula | C18H14N4OS | ||||||||||||
| Molar Mass | 334.39 | ||||||||||||
| Appearance | 固体 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Srivastava M, et al. An inhibitor of nonhomologous end-joining abrogates double-strand break repair and impedes cancer progression. Cell. 2012 Dec 21;151(7):1474-87. [2]. Lin C, et al. Increasing the Efficiency of CRISPR/Cas9-mediated Precise Genome Editing of HSV-1 Virus in Human Cells. Sci Rep. 2016 Oct 7;6:34531. [3]. Supriya V Vartak, et al. Autocyclized and Oxidized Forms of SCR7 Induce Cancer Cell Death by Inhibiting Nonhomologous DNA End Joining in a Ligase IV Dependent Manner. FEBS J. 2018 Nov;285(21):3959-3976. |