Table 1.
Fluorescence Polarization Assays Measuring Displacement of a FITC-BID Peptide From All Six Antiapoptotic Human BCL-2 Family Proteins to Compare IC50 Values of Small-Molecule BCL-2 Antagonists
| Protein | Compound IC50 (uM) |
||||||||
|---|---|---|---|---|---|---|---|---|---|
| EGCG | Gossypol | ApoG | Antimycin A | Chelerythrine | ABT-737 | Obatoclax | BH3I-1 | YC137 | |
| BCL-XL | 0.59 | 3.03 | 2.80 | 2.70 | Approximately 10 | 0.064 | 4.69 | 5.86 | > 20 |
| BCL-2 | 0.45 | 0.28 | 0.64 | 2.95 | Approximately 10 | 0.12 | 1.11 | 1.14 | 6.43 |
| BCL-w | 2.33 | 1.4 | 2.10 | 4.57 | > 10 | 0.024 | 7.01 | 2.33 | 2.21 |
| BCL-B | 0.36 | 0.16 | 0.37 | 1.83 | > 10 | > 10 | 2.15 | 1.08 | 3.10 |
| BFL-1 | 1.79 | > 10 | > 10 | > 10 | Approximately 10 | > 20 | 5.00 | 4.65 | > 20 |
| MCL-1 | 0.92 | 1.75 | 3.35 | 2.51 | > 10 | > 20 | 2.90 | 2.17 | 2.47 |
NOTE. Data adapted.26
Abbreviations: ApoG, apogossypol; BCL-2, B-cell lymphoma/leukemia 2; BCL-B, BCL-2–like protein 10; BCL-w, BCL-2–like protein 2; BCL-XL, BCL extra long; BFL-1, BCL-2–related gene expression in fetal liver; BH3I-1, BCL-2 homology 3 domain inhibitor 1; EGCG, epigallocatechin gallate; FITC, fluoresceine isothiocyanate; IC50, half maximal inhibitory concentration; MCL-1, myeloid cell leukemia 1.