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A-485 is a potent and selective HAT inhibitor of p300/CBP in vitro with an IC50 of 9.8 nM in a p300 TR-FRET assay and 2.6 nM in a CBP TR-FRET assay with selectivity > 1000-fold over closely related HATs. A-485 exhibits potent activity in most multiple myeloma cell lines, and in a subset of acute myeloid leukaemia lines and non-Hodgkin’s lymphoma lines. A-485 induces a comparable decrease in H3K27Ac in all five prostate cancer cell lines.
In tumour-bearing animals, dosing with A-485 for seven days induces a decrease in the mRNA levels of MYC and the AR-dependent gene SLC45A3 at three hours post-dosing, and (for MYC) a decrease in the protein level, indicating that A-485 inhibits p300-mediated transcriptional activity in vivo.
| Molecular Weight | 536.48 |
| Formula | C25H24F4N4O5 |
| CAS Number | 1889279-16-6 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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