Damnacanthal has > 100-fold selectivity for p56 over the serine/threonine kinases, protein kinase A and protein kinase C, and > 40-fold selectivity for p56 over four receptor tyrosine kinases. Damnacanthal also demonstrates modest (7-20-fold), but highly statistically significant, selectivity for p56 over the homologous enzymes p60 and p59.
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.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
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.
|