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Background: CREBBP (CBP) and EP300 are general transcriptional co-activators, which are involved in many biological processes like maintenance of genomic stability by affecting DNA replication and DNA repair as well as cell growth, transformation and development. They also play and essential role in neuronal plasticity/ memory formation hematopoiesis and energy homeostasis as demonstrated in a variety of mouse models. They possess both acetyl-transferase enzymatic and bromodomain containing regions. Through acetylation of non-histone proteins CREBBP can have a positive or negative effect on transcriptional regulation by affecting protein- protein interactions, protein-DNA interactions, nuclear retention or protein half-life.
Biological Activity: Inhibitor of CREBBP/EP300 bromodomains (IC50 values are 21-69 and 38 nM for CREBBP and EP300 bromodomains, respectively). Displays over 40-fold selectivity for CREBBP over BRD4. Accelerates FRAP recovery in cells at a concentration of 1 µM.
Description: Potent CREBBP/EP300 bromodomain inhibitor
Purity: ≥98% by HPLC
Solubility: Soluble in DMSO
Storage Stability: Store at or below +4°C. Solid form is stable at least 12 months from date of receipt, when stored as directed.
Target: CREBBP, p300
Biosafety Level: Not applicable (BSL-1)
References: Gallenkamp et al. (2014). Chem Med Chem 9:438.
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