Biological Activity
Selective CBP/p300 bromodomain inhibitor (IC50 values are 125 and 363 nM, respectively). Exhibits >100-fold selectivity for CBP over BRD4. Also exhibits selectivity over a panel of other bromodomains. Reduces LPS-induced IL-1β, IL-6 and IFN-β expression in macrophages in vitro. Also downregulates RGS4 expression in primary cortical neurons in vitro.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
External Portal Informaiton
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of PF CBP1 is reviewed on the chemical probes website.
Technical Data
| M. Wt | 488.62 |
| Formula | C29H36N4O3 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1962928-21-7 |
| PubChem ID | 119081417 |
| InChI Key | CGWBJJZOKGZCSJ-UHFFFAOYSA-N |
| Smiles | CC(ON=C1C)=C1C2=CC(N=C(CCC3=CC=C(OCCC)C=C3)N4CCN5CCOCC5)=C4C=C2 |
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 | 48.86 | 100 | |
| ethanol | 48.86 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 488.62. 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 | 2.05 mL | 10.23 mL | 20.47 mL |
| 5 mM | 0.41 mL | 2.05 mL | 4.09 mL |
| 10 mM | 0.2 mL | 1.02 mL | 2.05 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.41 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Chekler et al (2015) Transcriptional profiling of a selective CREB binding protein bromodomain inhibitor highlights therapeutic opportunities. Chem.Biol. 22 1588 PMID: 26670081
Keywords: PF CBP1, supplier, PFCBP1, selective, CBP, CREBBP, EP300, bromodomains, inhibitors, inhibits, Bromodomains, Bromodomains, Tocris Bioscience
