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。
| 生物活性 | SCR7 pyrazine is aDNA ligase IVinhibitor that blocksnonhomologous end-joining (NHEJ)in a ligase IV-dependent manner. SCR7 pyrazine is also aCRISPR/Cas9enhancer which increases the efficiency of Cas9-mediated homology-directed repair (HDR). SCR7 pyrazine induces cellapoptosisand has anticancer activity[1][2]. |
| IC50& Target | DNA Ligase IV[1]
CRISPR/Cas9[2] |
体外研究
(In Vitro) | SCR7 pyrazine (20-100 μM; 24 hours; MCF7 cells) treatment interferes with NHEJ in cells, leading to accumulation of unrepaired double-strand breaks (DSBs)[1].
SCR7 pyrazine treatment shows a dose-dependent decrease in cell proliferation with IC50values 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[1].
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[1].
Western Blot Analysis[1] | Cell Line: | MCF7 cells | | Concentration: | 20 μM, 40 μM, 100 μM | | Incubation Time: | 24 hours | | Result: | Showed an increase in levels of gH2AX foci and protein. |
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体内研究
(In Vivo) | SCR7 pyrazine (10 mg/kg; intraperitoneal injection; six doses; BALB/c mice) treatment significantly reduces breast adenocarcinoma-induced tumor and increases lifespan[1].
| Animal Model: | BALB/c mice injected with breast adenocarcinoma cells[1] | | Dosage: | 10 mg/kg | | Administration: | Intraperitoneal injection; on alternate days (0, 2, 4, 6, 8, and 10) | | Result: | Significantly reduced breast adenocarcinoma-induced tumor and increased lifespan. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(300.86 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.0086 mL | 15.0430 mL | 30.0860 mL | | 5 mM | 0.6017 mL | 3.0086 mL | 6.0172 mL | | 10 mM | 0.3009 mL | 1.5043 mL | 3.0086 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (7.52 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.52 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (7.52 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.52 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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