产品描述: | L67 (DNA Ligase Inhibitor) is a competitive DNA ligase inhibitor that effectively inhibits DNA ligases I/III (both IC50 are 10 μM). L67 (DNA Ligase Inhibitor) can cause nuclear DNA damage by reducing levels of mitochondrial DNA and increasing levels of mitochondrially-generated ROS. L67 (DNA Ligase Inhibitor) also activates the Caspase 1-dependent apoptosis pathway in cancer cells, can be used in cancer research |
靶点: |
DNA/RNA Synthesis;Caspase;Apoptosis;Reactive Oxygen Species;DNA;DNA/RNASynthesis |
体外研究: |
L67 (10, 15 μM; 24 h) promotes nuclear DNA damage and (0-50 μM) increases level of mSOX by inhibiting mitochondrial LigIIIα in HeLa cells. L67 (10 μM; 24 h) induces changes in mitochondrial function that causes a reduction in OCR and mitochondrial DNA, and abnormal mitochondrial morphology in HeLa. L67 (10, 100 μM; 24 h) induces apoptosis in cancer cells. L67 (0-30 μM; 24 h) selectively induces cell death in cancer cells by activating a caspase 1-dependent apoptotic pathway. Cell Viability Assay Cell Line: HeLa cells Concentration: 10, 15 μM; 0-50 μM Incubation Time: 24 h Result: Increased the formation of nuclear γH2AX foci and steady state levels of γH2AX when at 10 or 15 μM. (γH2AX: a sign of DNA double-strand breaks).Resulted in a concentration (0-50 μM)-dependent increase in mSOX (mitochondrial superoxide) levels. (mSOX is a major cause of the cellular oxidative damage). Cell Viability Assay Cell Line: HeLa cells Concentration: 10 μM Incubation Time: 24 h Result: Reduced oxygen consumption rate (OCR) approximately 20%.Resulted in about a 25% reduction in mitochondrial DNA. Apoptosis Analysis Cell Line: HeLa cells Concentration: 10, 100 μM Incubation Time: 24 h Result: Result:Induced apoptosis, and at 100 μM with apoptotic cells constituting about 50% of the HeLa cell population. Cell Viability Assay Cell Line: HeLa cells Concentration: 0-30 μM Incubation Time: 24 h Result: Activates a caspase 1-dependent cell death pathway in cancer cells. |
参考文献: |
1. Sallmyr A, et al. Inhibiting Mitochondrial DNA Ligase IIIα Activates Caspase 1-Dependent Apoptosis in Cancer Cells. Cancer Res. 2016 Sep 15;76(18):5431-41. 2. Chen X, et al. Rational design of human DNA ligase inhibitors that target cellular DNA replication and repair. Cancer Res. 2008 May 1;68(9):3169-77. |
溶解性: |
Soluble in DMSO、H2O |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.057 ml |
10.286 ml |
20.571 ml |
5 mM |
0.411 ml |
2.057 ml |
4.114 ml |
10 mM |
0.206 ml |
1.029 ml |
2.057 ml |
50 mM |
0.041 ml |
0.206 ml |
0.411 ml |
|
注意: |
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