PF CBP1

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Cat.No. 5801 - PF CBP1 | C29H36N4O3 | CAS No. 1962928-21-7
Description: Selective CBP/p300 bromodomain inhibitor
Chemical Name: 5-(Dimethyl-1,2-oxazol-4-yl)-1-[2-(morpholin-4-yl)ethyl]-2-[2-(4-propoxyphenyl)ethyl]-1H-1,3-benzodiazole
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

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.

Negative Control also available.

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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the biological activity of the product.

Chekler et al (2015) Transcriptional profiling of a selective CREB binding protein bromodomain inhibitor highlights therapeutic opportunities. Chem.Biol. 22 1588 PMID: 26670081


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Citations for PF CBP1

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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* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Epigenetics

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.

Epigenetics

Epigenetics Research Bulletin

Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:

  • Bromodomains
  • DNA Methyltransferases
  • Histone Deacetylases
  • Histone Demethylases
  • Histone Methyltransferases
Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.