A 485

Pricing Availability   Qty
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)
Datasheet
Citations (13)
Reviews
Literature (1)

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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.

View Related Products by Target

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View all Histone Acetyltransferase Inhibitors

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:

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

Lynda K et al (2022) A mitotic chromatin phase transition prevents perforation by microtubules. Nature 609 183-190 PMID: 35922507

Adriana et al (2022) 3D chromatin remodeling potentiates transcriptional programs driving cell invasion. Proc Natl Acad Sci U S A 119 e2203452119 PMID: 36037342


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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.


Epigenetics Scientific Review

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.