Compound class:
Synthetic organic
Comment: I-CBP112 is an inhibitor of the bromodomain-containing proteins CREB binding protein (CREBBP) and E1A binding protein p300 (EP300) and was developed by the Structural Genomics Consortium (SGC) [3]. The bromodomains facilitate binding of these proteins to acetylated lysine residues on histones and other proteins [4], interactions which underlie the function of these two transctiptional co-activators in the control of DNA replication and repair, cell growth, transformation, and development [1-2].
Click here to link to the SGC's full list of epigenetics probes. Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
|
References |
1. Iyer NG, Ozdag H, Caldas C. (2004)
p300/CBP and cancer. Oncogene, 23 (24): 4225-31. [PMID:15156177] |
2. Kalkhoven E. (2004)
CBP and p300: HATs for different occasions. Biochem Pharmacol, 68 (6): 1145-55. [PMID:15313412] |
3. SGC.
I-CBP112 A CREBBP/EP300-selective chemical probe. Accessed on 04/08/2023. Modified on 04/08/2023. thesgc.org, https://www.thesgc.org/chemical-probes/I-CBP112 |
4. Zeng L, Zhang Q, Gerona-Navarro G, Moshkina N, Zhou MM. (2008)
Structural basis of site-specific histone recognition by the bromodomains of human coactivators PCAF and CBP/p300. Structure, 16 (4): 643-52. [PMID:18400184] |