Potency data for probe A-485 and control A-486
In vitro potency
| Target name | Target information | Species | Assay description | A-485 | A-486 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| EP300 | BHC (bromodomain-HAT-C/H3) domain | Homo sapiens | Time-resolved fluorescence energy transfer (TR-FRET) measuring acetylation of a biotinylated histone H4 peptide (EP300) | IC50 = 9.8 nM | IC50 > 10000 nM | PMID: 28953875 |
| CREBBP | BHC (bromodomain-HAT-C/H3) domain | Homo sapiens | Time-resolved fluorescence energy transfer (TR-FRET) measuring acetylation of a biotinylated histone H4 peptide (CREBBP) | IC50 = 2.6 nM | IC50 = 9032 nM | PMID: 28953875 |
| EP300 | HAT domain | Homo sapiens | Surface plasmon resonance (Biocore) | KD = 15 nM ± 1.000 nM | KD = 20000 nM ± 1000.000 nM | PMID: 28953875 |
In cell potency
| Target name | Target information | Species | Assay description | A-485 | A-486 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| Androgen dependent LnCaP-FGC cell line (prostate cancer) | Homo sapiens | Inhibition of H3K27Ac (LnCaP-FGC) | IC50 = 150 nM | IC50 > 10 µM | PMID: 28953875 | |
| DU-145 cell line (prostate cancer) | Homo sapiens | Inhibition of H3K27Ac (DU-145) | IC50 = 136 nM | IC50 > 10 µM | PMID: 28953875 | |
| Androgen dependent LnCaP-FGC cell line (prostate cancer) | Homo sapiens | LnCaP-FGC Proliferation | IC50 = 381 nM | IC50 > 10 µM | PMID: 28953875 | |
| DU-145 cell line (prostate cancer) | Homo sapiens | DU-145 Proliferation | IC50 > 10 µM | IC50 > 10 µM | PMID: 28953875 |