A 485

Key Product Details

Product Description

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.

Product Specifications for A 485

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

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

2 1 Recalculate

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

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 63 publications citing the usage of this 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

Product Documents for A 485