SGC-CBP30
Catalog #
27650-1
$220
*
●
●
Purchase
Description
Potent CREBBP/EP300 bromodomain inhibitor
●
Synonyms
SGCCBP30; SGC CBP30; 4-[(2S)-1-[2-[2-(3-chloro-4-methoxyphenyl)ethyl]-5-(3,5-dimethyl-1,2-oxazol-4-yl)benzimidazol-1-yl]propan-2-yl]morpholine
●
Product Data Gallery
Product Info
Storage and Usage
Citations
Purity
≥98% by HPLC
Target(s)
CREBBP, p300
Formula
C28H33ClN4O3
MW
509.0 Da
Solubility
Soluble in DMSO
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.
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.
References
Gallenkamp et al. (2014). Chem Med Chem 9:438.
Powered by Bioz
6405 Mira Mesa Blvd. Suite 100
San Diego, CA 92121
858-202-1401
San Diego, CA 92121
858-202-1401
Products are for Research Use Only
COMPANY
Copyright © 2024
BPS Bioscience, Inc.
All rights reserved.
Diagrams on this website are created with BioRender.com.