SCR7 pyrazine 是一种 DNA 连接酶 IV (DNA ligase IV) 抑制剂，它以连接酶 IV 依赖的方式阻断非同源末端连接 (NHEJ)。SCR7 pyrazine 也是一种 CRISPR/Cas9 的增强子，可提高 Cas9 介导的同源性定向修复 (HDR) 的效率。SCR7 pyrazine 诱导细胞凋亡 (apoptosis) 并具有抗癌活性。
| CAS No. | 14892-97-8 |
| 生物活性 | 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. |
| 分子式 | C18H12N4Os |
| 分子量 | 332.38 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存条件 | Powder -20°C 3 years |
| 溶解性数据 | DMSO : 100 mg/mL (300.86 mM; Need ultrasonic) |
| 体内研究 | SCR7 pyrazine (10 mg/kg; intraperitoneal injection; six doses; BALB/c mice) treatment significantly reduces breast adenocarcinoma-induced tumor and increases lifespan. |
| 体外研究 | SCR7 pyrazine (20-100 μM; 24 hours; MCF7 cells) treatment interferes with NHEJ in cells, leading to accumulation of unrepaired double-strand breaks (DSBs). SCR7 pyrazine treatment shows a dose-dependent decrease in cell proliferation with IC50 values of 40 μM, 34 μM, 44 μM, 8.5 μM, 120 μM, 10 μM and 50 μM for MCF7, A549, HeLa, T47D, A2780, HT1080 and Nalm6 cells, respectively. In MCF7 cells, SCR7 pyrazine (20, 40 μM) treatment increases phosphorylation of ATM and activates p53, decreases MDM2, BCL2, resulting in activation of proapoptotic proteins, PUMA and BAX. And the shorter fragments of MCL1, PARP1, Caspase 3, and Caspase 9 cleavage are upregulated in a dose-dependent manner. |
| 纯度及产品资料 | 98% |
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