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Submit ReviewSelective 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.
Sold for research purposes under agreement from Pfizer Inc.
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.
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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
Keywords: PF CBP1, PF CBP1 supplier, PFCBP1, selective, CBP, CREBBP, EP300, bromodomains, inhibitors, inhibits, Bromodomains, 5801, Tocris Bioscience
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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.
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.