A 485

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Cat.No. 6387 - A 485 | C25H24F4N4O5 | CAS No. 1889279-16-6
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
Reviews
Literature

Biological Activity

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). Displays > 1000-fold selectivity over closely related HATs. Suppresses proliferation in several hematological malignancies and AR+ prostate cancer cell lines in vitro. Inhibits tumor growth in a castration-resistant prostate cancer xenograft model. 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.

Technical Data

M. Wt 536.48
Formula C25H24F4N4O5
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1889279-16-6
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.

All Tocris products are intended for laboratory research use only.

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 solvent 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

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


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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

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