hCAIX/XII-IN-5 (Coumarin 9a) 是一种碳酸酐酶 (CA) 抑制剂，并表现出比对 hCA I 和 hCA II 极佳的 hCA IX/XII 选择性 (Ki分别为 93.9 和 85.7 nM)。hCAIX/XII-IN-5 对癌细胞显示出抗增殖活性。hCAIX/XII-IN-5 能延迟细胞周期并诱导细胞的凋亡。
| 生物活性 | hCAIX/XII-IN-5 (Coumarin 9a) acarbonic anhydrase(CA) inhibitor, and exhibits excellent hCA IX/XII selectivity (Ki=93.9 and 85.7 nM, respectively) over hCA I and hCA II. hCAIX/XII-IN-5 shows anti-proliferative activities tocancercells. hCAIX/XII-IN-5 can delay cell cycle and induceapoptosis[1]. |
| IC50& Target | hCA IX 93.9 nM (Ki) | hCA XII 85.7 nM (Ki) |
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体外研究
(In Vitro) | hCAIX/XII-IN-5 (2.36-32.17 μM) treatment shows both anti-proliferative activities to MCF-7 and PANC-1 cells under the normoxic and hypoxic condition[1].
hCAIX/XII-IN-5 (2.69 μM; 24 h) treatment shows accumulation of MCF-7 cells in the Sub-G1phase and cell arrest in G2-M phase[1].
hCAIX/XII-IN-5 (2.69 μM; 24 h) treatment increases the percent of annexin V-FITC-positive apoptotic cells, including both the early and late apoptotic cells (UR+LR)[1].
Cell Proliferation Assay[1] | Cell Line: | MCF-7 and PANC-1 cells | | Concentration: | 2.36-32.17 μM | | Incubation Time: | | | Result: | Exerted anti-proliferative activities to MCF-7 and PANC-1 cells (IC50=2.69 μM and 32.17 μM, respectively) under the normoxic condition, and moderate activitits against both MCF-7 and PANC-1 cells (IC50=16.36 μM and 11.78 μM, respectively) under the hypoxic condition. |
Cell Cycle Analysis[1] | Cell Line: | MCF-7 cells | | Concentration: | 2.69 μM | | Incubation Time: | 24 hours | | Result: | Resulted in a significant increase in the percentage of cells at Sub-G1by 14-folds with significant increase in cell percentage in the G1-M phase by 2.3-folds compared to the control. |
Apoptosis Analysis[1] | Cell Line: | MCF-7 cells | | Concentration: | 2.69 μM | | Incubation Time: | 24 hours | | Result: | Resulted in a significant increase in the percent of annexin V-FITC-positive apoptotic cells, including both the early (from 0.61% to 6.77%) and late apoptotic (from 0.27% to 14.84%) cells (UR+LR), about 11- and 55-fold increase, respectively, as compared with the control. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
