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Description: Potent and selective p300/CBP inhibitor; orally bioavailable
Chemical Name: (1R)-N-[(4-Fluorophenyl)methyl]-2,3-dihydro-5-[[(methylamino)carbonyl]amino]-2',4'-dioxo-N-[(1S)-2,2,2-trifluoro-1-methylethyl]spiro[1H-indene-1,5'-oxazolidine]-3'-acetamide
Purity: ≥98% (HPLC)
Biological Activity
A 485 is a potent and selective p300/CREB-binding protein (CBP) HAT domain inhibitor (IC50 values are 2.6 and 9.8 nM for the CBP-bromodomain HAT-C/H3 (BHC) and p300-BHC domains, respectively), which displays > 1000-fold selectivity over closely related HATs. A 485 suppresses proliferation in several hematological malignancies and AR+ prostate cancer cell lines in vitro, and also inhibits tumor growth in a castration-resistant prostate cancer xenograft model. A 485 is orally bioavailable.
To request the negative control for A 485, please fill out the A 486 request form on the SGC website.
Licensing Information
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the A-485 probe summary on the SGC website.
External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of A 485 is reviewed on the chemical probes website.
Compound Libraries
A 485 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 536.48 |
| Formula | C25H24F4N4O5 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1889279-16-6 |
| PubChem ID | 118958122 |
| InChI Key | VRVJKILQRBSEAG-LFPIHBKWSA-N |
| Smiles | CNC(NC1=CC=C2C(CC[C@@]23OC(N(C3=O)CC(N([C@H](C(F)(F)F)C)CC4=CC=C(C=C4)F)=O)=O)=C1)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 53.65 | 100 | |
| ethanol | 53.65 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 536.48. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.86 mL | 9.32 mL | 18.64 mL |
| 5 mM | 0.37 mL | 1.86 mL | 3.73 mL |
| 10 mM | 0.19 mL | 0.93 mL | 1.86 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.37 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Lasko et al (2017) Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours. Nature 550 128 PMID: 28953875
Kodadek et al (2018) Another one (of the "undruggable" targets) bites the dust: discovery of a potent and selective inhibitor of the histone acetyl transferase p300/CBP. Biochemistry 57 899 PMID: 29244478
Weinert et al (2018) Time-Resolved Analysis Reveals Rapid Dynamics and Broad Scope of the CBP/p300 Acetylome. Cell. PMID: 29804834
If you know of a relevant reference for A 485, please let us know.
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Keywords: A 485, A 485 supplier, A485, inhibitors, inhibits, histone, acetyltransferase, HAT, PCAF, p300, HSCs, potent, selective, androgen, receptor-positive, prostate, CBP, Histone, Acetyltransferases, 6387, Tocris Bioscience
Citations for A 485
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Cancer Research Product Guide
A collection of over 750 products for cancer research, the guide includes research tools for the study of:
- Cancer Metabolism
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- Receptor Signaling
- Cell Cycle and DNA Damage Repair
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Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Epigenetics Research Bulletin
Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:
- Bromodomains
- DNA Methyltransferases
- Histone Deacetylases
- Histone Demethylases
- Histone Methyltransferases