All AbMole products are for research use only, cannot be used for human consumption.
A-485 is a potent and selective HAT inhibitor of p300/CBP in vitro with an IC50 of 10 nM in a p300 TR-FRET assay and 3 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 ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Histone Acetyltransferase Products |
|---|
| CBP/p300-IN-5
P300/CBP-IN-5 is a potent p300/CBP histone acetyltransferase inhibitor, has an IC50 of 18.8 nM. |
| JG-2016
JG-2016 is a potent inhibitor of histone acetyltransferase 1 (HAT1), with an IC50 of 14.8 μM in the HAT1 acetylation assays. |
| AU-18069
AU-18069 is a CBP/p300 HAT inhibitor that can be used in studies related to hematological and solid tumors. |
| KAT modulator-1
KAT modulator-1 is a KAT modulator. |
| KAT6-IN-1
KAT6-IN-1 is a potent KAT6 inhibitor. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
