A 485

Name: A 485
Brand: Tocris Bioscience
SKU: 6387

Tocris Bioscience, part of Bio-Techne | Catalog # 6387

Citations (46)

COA / SDS

Potent and selective p300/CBP inhibitor; orally bioavailable

Key Product Details

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)
Molecular Weight:	536.48

View Full Technical Details for A 485

Technical Data
Citations

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.

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.

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.

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 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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References for A 485

References are publications that support the biological activity of the product.

Kodadek Another one (of the "undruggable" targets) bites the dust: discovery of a potent and selective inhibitor of the histone acetyl transferase p300/CBP. Biochemistry 2018 PMID: 29244478
Weinert Time-Resolved Analysis Reveals Rapid Dynamics and Broad Scope of the CBP/p300 Acetylome. Cell. 2018 PMID: 29804834
Lasko Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours. Nature 2017 PMID: 28953875