A 485
Tocris Bioscience, part of Bio-Techne | Catalog # 6387
Potent and selective p300/CBP inhibitor; orally bioavailable
Key Product Details
Description
Potent and selective p300/CBP inhibitor; orally bioavailable
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
Molecular Weight
536.48
Formula
C25H24F4N4O5
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for A 485
For research use only
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