中文名 | 丹宁卡 |
英文名 | Damnacanthal |
别名 | 丹宁卡 丹拿堪索 3-羟基-1-甲氧基-2-蒽醌甲醛 丹宁卡【3-羟基-1-甲氧基-2-蒽醌甲醛】 |
英文别名 | DAMNACANTAL Damnacanthal DAMNACANTHAL 3-HYDROXY-1-METHOXYANTHRAQUINONE-2-ALDEHYDE 1-Methoxy-2-formyl-3-hydroxy-9,10-anthraquinone 1-Methoxy-3-hydroxy-9,10-dioxoanthracene-2-carbaldehyde 1-Methoxy-3-hydroxy-9,10-dioxo-9,10-dihydroanthracene-2-carbaldehyde 9,10-Dihydro-3-hydroxy-1-methoxy-9,10-dioxo-2-anthracenecarbaldehyde 9,10-Dihydroxy-3-hydroxy-1-methoxy-9,10-dioxo-2-anthracenecarboxaldehyde |
CAS | 477-84-9 |
化学式 | C16H10O5 |
分子量 | 282.25 |
密度 | 1.461±0.06 g/cm3(Predicted) |
熔点 | 218~219℃ |
沸点 | 531.9±50.0 °C(Predicted) |
溶解度 | 溶于DMSO (高达7 mg/ml) |
酸度系数 | 5.26±0.20(Predicted) |
存储条件 | -20°C |
稳定性 | 自供应购买之日起稳定1年。DMSO中的溶液可以在-20 °C下保存长达1个月。 |
外观 | 淡橙色固体。 |
颜色 | Yellow |
体外研究 | Damnacanthal has > 100-fold selectivity for p56 lck over the serine/threonine kinases, protein kinase A and protein kinase C, and > 40-fold selectivity for p56 lck over four receptor tyrosine kinases. Damnacanthal also demonstrates modest (7-20-fold), but highly statistically significant, selectivity for p56 lck over the homologous enzymes p60 src and p59 fyn . Damnacanthal (0.1-100 μM; 1-4 days; HCT-116 and SW480 cells) treatment results in a significant reduction of cell proliferation in a concentration- and time-dependent manner. Damnacanthal (1-50 μM; 72 hours; HCT-116 cells) treatment results in a significant enrichment in the number of cells in the S/G1 and G2/G1 phases at concentration of 50 μM. Damnacanthal (10 μM; 24 hours; HCT-116 cells) treatment significantly increases caspase 3/7 activity. Damnacanthal-induced apoptosis. Damnacanthal (0.1-10 μM; 24 hours; HCT-116 cells) treatment induces NAG-1 expression in HCT-116 cells. Cyclin D1 expression is reduced at 10 μM of Damnacanthal, whereas p21 and p53 does not alter their expression. PARP cleavage is seen at 10 μM Damnacanthal treatment only in HCT-116 cells, where NAG-1 is induced. Damnacanthal treatment for 2 weeks shows significant decreasing colony number in HCT-116 cells in a concentration-dependent manner. Damnacanthal-treated cells show a dramatic inhibition of clonogenic capacity. Damnacanthal-treated (1-50 μM; 48 hours) cells significantly inhibits the migration of HCT-116 cells in a concentration-dependent manner. Cell Proliferation Assay Cell Line: HCT-116 and SW480 cells Concentration: 0.1 μM, 1 μM, 10 μM, 100 μM Incubation Time: 1, 2, and 4 days Result: Resulted in a significant reduction of cell proliferation in a concentration- and time-dependent manner. Cell Cycle Analysis Cell Line: HCT-116 cells Concentration: 1 μM, 10 μM and 50 μM Incubation Time: 72 hours Result: Resulted in a significant enrichment in the number of cells in the S/G1 and G2/G1 phases at concentration of 50 μM. Apoptosis Analysis Cell Line: HCT-116 cells Concentration: 10 μM Incubation Time: 24 hours Result: Significantly increased caspase 3/7 activity. Western Blot Analysis Cell Line: HCT-116 cells Concentration: 0.1 μM, 1 μM and 10 μM Incubation Time: 24 hours Result: NAG-1 was induced in HCT-116 cells in a dose- and time-dependent manner. Cyclin D1 expression was reduced at 10 μM. |
体内研究 | Damnacanthal (10-100 mg/kg; oral administration; for 10-300 minutes; male ddY mice) treatment exhibits a significant antinociceptive effect in a dose-dependent manner in the formalin test. Administration of damnacanthal (100 mg/kg) shows significant inhibition of histamine-induced paw edema. Animal Model: Male ddY mice (5-6 weeks) injected with formalin or Histamine Dosage: 10 mg/kg, 30 mg/kg and 100 mg/kg Administration: Oral administration; for 10 minutes, 30 minutes, 60 minutes or 300 minutes Result: Significantly reduced the growth of human lung tumor without acute toxicity. |
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