Effects of MCL-1 ASO and various inhibitory drugs on 3H-thymidine uptake (IC50) and induction of apoptosis (EC50) in HMC-1.1 cells and HMC-1.2 cells
| Compound . | 3H-thymidine uptake (IC50) . | Apoptosis (EC50) . | ||
|---|---|---|---|---|
| HMC-1.1 . | HMC-1.2 . | HMC-1.1 . | HMC-1.2 . | |
| MCL-1 ASO | 40-80 nM | 60-100 nM | 250 nM | > 250 nM |
| PKC412 | 50-250 nM | 50-250 nM | 0.5-3 μM | 0.5-3 μM |
| AMN107 | 3-10 nM | 1-3 μM | 30-80 nM | > 10 μM |
| Imatinib | 10-30 nM | > 3 μM | 50-150 nM | > 10 μM |
| 2CdA | 0.1-0.3 μg/mL | 5-20 ng/mL | > 1 μg/mL | > 1 μg/mL |
| Compound . | 3H-thymidine uptake (IC50) . | Apoptosis (EC50) . | ||
|---|---|---|---|---|
| HMC-1.1 . | HMC-1.2 . | HMC-1.1 . | HMC-1.2 . | |
| MCL-1 ASO | 40-80 nM | 60-100 nM | 250 nM | > 250 nM |
| PKC412 | 50-250 nM | 50-250 nM | 0.5-3 μM | 0.5-3 μM |
| AMN107 | 3-10 nM | 1-3 μM | 30-80 nM | > 10 μM |
| Imatinib | 10-30 nM | > 3 μM | 50-150 nM | > 10 μM |
| 2CdA | 0.1-0.3 μg/mL | 5-20 ng/mL | > 1 μg/mL | > 1 μg/mL |
3H-thymidine uptake was analyzed after 24 hours of incubation with drugs or transfection with ASO, and the percentage of apoptotic cells was determined on cytospin preparations after cells had been incubated with drugs for 24 hours. For evaluation of apoptosis, cells were examined 12 hours after transfection with ASO. After 24 hours, the number of apoptotic cells was greater than 50% in all instances (IC50, mean inhibitory concentration; EC50, mean effective concentration).