| Name | A-485 |
| Description | A-485 is a potent and selective catalytic p300/CBP inhibitor with IC50 values of 9.8 nM for p300 and 2.6 nM for CBP. |
| In vitro | METHODS: 124 tumor cells were treated with A-485 for 3-5 days and cell viability was measured by the CellTiter-Glo Luminescent Cell Viability Assay.
RESULTS: The broadest sensitivity was observed in hematologic tumors, where A-485 exhibited potent activity in most multiple myeloma (MM) cell lines, acute myeloid leukemia (AML) cell lines, and non-Hodgkin's lymphoma (NHL) cell lines. In contrast, several solid tumor lines, including melanoma, small cell lung cancer (SCLC), and triple-negative breast cancer (TNBC), showed significantly reduced sensitivity to A-485. [1]
METHODS: H1650 and H1650-ER cells were treated with A-485 (20 µM) overnight, followed by TRAIL (10-100 ng/mL) overnight, and apoptosis was detected by apoptotic kit.
RESULTS: The combination of A-485 and TRAIL significantly increased the total number of apoptotic cells in H1650 and H1650-ER cells compared to TRAIL alone.A-485 enhanced TRAIL-induced apoptosis. [2] |
| In vivo | METHODS: To assay in vivo anti-tumor activity, A-485 (100 mg/kg) was administered intraperitoneally twice daily for 21 days to SCID mice bearing LuCaP-77 CR xenografts.
RESULTS: A-485 induced 54% tumor growth inhibition (TGI) after 21 days of administration. [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (9.32 mM), Sonication is recommended.
DMSO : 252.5 mg/mL (470.66 mM), Sonication is recommended.
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| Keywords | p300 | Inhibitor | inhibit | HistoneAcetyltransferase | histone acetyltransferase | HATs | HAT | EpigeneticReaderDomain | Epigenetic Reader Domain | CBP/p300 | CBP | A-485 | A485 | A 485 |
| Inhibitors Related | ABBV-744 | SNDX-5613 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | Acetaminophen | 5-Ph-IAA | Manganese chloride (tetrahydrate) | Curcumin | N4-Acetylcytidine | Naphthol AS-E | JQ-1 (carboxylic acid) | Bisdemethoxycurcumin |
| Related Compound Libraries | Reprogramming Compound Library | Bioactive Compound Library | Epigenetics Compound Library | Inhibitor Library | Anti-Prostate Cancer Compound Library | NO PAINS Compound Library | Stem Cell Differentiation Compound Library | PPI Inhibitor Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
