Table 1. NOXA Derived Peptide Sequences and Relative IC50 Values in a DELFIA Assay against the Bcl-2 Family Proteins hBfl-1, hMcl-1, hBcl-xL, and hBcl-2a.
| DELFIA IC50 (nM) |
|||||
|---|---|---|---|---|---|
| compd ID | aa sequence | hBfl-1 | hMcl-1 | hBcl-xL | hBcl-2 |
| hNOXA | Ac-CATQLRRFGDKLNFRQKLLN-NH2 | 7.5 ± 2 | 228 ± 1 | >1 μM | >1 μM |
| homo_hNOXA | Ac-hCATQLRRFGDKLNFRQKLLN-NH2 | 83 ± 11 | 266 ± 31 | >1 μM | >1 μM |
| λ_hNOXA | Ac-λATQLRRFGDKLNFRQKLLN-NH2 | 287 ± 69 | 233 ± 25 | >1 μM | >1 μM |
| hNOXAs | Ac-CATQLRRFGDKLN-NH2 | 15 ± 2 | >1 μM | >1 μM | >1 μM |
| NOXA A | Ac-AELPPEFAAQLRKIGDKVYC-NH2 | >1 μM | 450 ± 1 | >1 μM | >1 μM |
| NOXA B | Ac-PADLKDECAQLRRIGDKVNL-NH2 | 431 ± 35 | 479 ± 28 | >1 μM | >1 μM |
| C1A_hNOXAs | Ac-AATQLRRFGDKLN-NH2 | >1 μM | >1 μM | n.t. | n.t. |
| cyc_hNOXA | Ac-CATQLRRFGDKLNFRQKLLNLISKLFC-NH2 | 86 ± 13 | 344 ± 41 | n.t. | n.t. |
a
hC = homocysteine; λ = Dap-2-chloroacetamide; C1–C27 in cyc-NOXA = disulfide bridge. n.t.: not tested. Values are the results of multiple measurements run in duplicates and represent the mean ± SE.