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。

hCAIX/XII-IN-5 (Coumarin 9a) a carbonic anhydrase ( CA ) inhibitor, and exhibits excellent hCA IX/XII selectivity ( K i =93.9 and 85.7 nM, respectively) over hCA I and hCA II. hCAIX/XII-IN-5 shows anti-proliferative activities to cancer cells. hCAIX/XII-IN-5 can delay cell cycle and induce apoptosis [1].

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-G 1 phase and cell arrest in G 2 -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 (IC 50 =2.69 μM and 32.17 μM, respectively) under the normoxic condition, and moderate activitits against both MCF-7 and PANC-1 cells (IC 50 =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-G 1 by 14-folds with significant increase in cell percentage in the G 1 -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.

C18H13NO3

291.3

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years