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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 for A 485
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 for A 485
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 for A 485
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 for A 485
| 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 for A 485
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 53.65 | 100 | |
| ethanol | 53.65 | 100 |
Preparing Stock Solutions for A 485
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 for A 485
References for A 485
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
13 Citations for A 485
Citations are publications that use Tocris products. Selected citations for A 485 include:
Peggie et al (2021) The single-cell epigenomic and transcriptional landscape of immunity to influenza vaccination. Cell 184 3915-3935.e21 PMID: 34174187
Johan et al (2021) The transcriptional coactivator CBP/p300 is an evolutionarily conserved node that promotes longevity in response to mitochondrial stress. Nat Aging 1 165-178 PMID: 33718883
Rebecca et al (2021) Nuclear ADP-ribosylation drives IFNγ-dependent STAT1α enhancer formation in macrophages. Nat Commun 12 3931 PMID: 34168143
Marc et al (2021) Extracellular signal-regulated kinase mediates chromatin rewiring and lineage transformation in lung cancer. Elife 10 PMID: 34121659
Hubertus et al (2021) A unique bipartite Polycomb signature regulates stimulus-response transcription during development. Nat Genet 53 379-391 PMID: 33603234
Aristotelis et al (2021) H3K27ac bookmarking promotes rapid post-mitotic activation of the pluripotent stem cell program without impacting 3D chromatin reorganization. Mol Cell 81 1732-1748.e8 PMID: 33730542
Adriana et al (2022) 3D chromatin remodeling potentiates transcriptional programs driving cell invasion. Proc Natl Acad Sci U S A 119 e2203452119 PMID: 36037342
Anusha et al (2022) Oncohistone Mutations Occur at Functional Sites of Regulatory ADP-Ribosylation. Cancer Res 82 2361-2377 PMID: 35472077
Lynda K et al (2022) A mitotic chromatin phase transition prevents perforation by microtubules. Nature 609 183-190 PMID: 35922507
Asgerally T et al (2020) ARID1A Mutations Promote P300-Dependent Endometrial Invasion through Super-Enhancer Hyperacetylation. Cell Rep 33 108366 PMID: 33176148
Masaya et al (2020) Acetylation-dependent regulation of PD-L1 nuclear translocation dictates the efficacy of anti-PD-1 immunotherapy. Nat Cell Biol 22 1064-1075 PMID: 32839551
Jing et al (2019) The Acetylation of Lysine-376 of G3BP1 Regulates RNA Binding and Stress Granule Dynamics. Mol Cell Biol 39 PMID: 31481451
Stephen J et al (2019) Clinically Advanced p38 Inhibitors Suppress DUX4 Expression in Cellular and Animal Models of Facioscapulohumeral Muscular Dystrophy. J Pharmacol Exp Ther 370 219-230 PMID: 31189728
Do you know of a great paper that uses A 485 from Tocris? Please let us know.
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Cancer Research Product Guide
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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.