SGC-CBP30 is a highly potent and selective p300/CBP bromodomain inhibitor (IC₅₀ ~0.021-0.069 µM for CBP and ~0.038 µM for p300). It has 40-fold selectivity for CBP over BRD4. It accelerated FRAP recovery at 1 µM. p300 and CBP are transcriptional co-activators that modulate DNA replication, DNA repair, cell growth, transformation, and development. Both p300 and CBP contain bromodomains, which mediate their binding to acetylated lysine residues on histones and other proteins. Chromosomal translocations of p300 or CBP with MOZ, MLL have been observed in acute myeloid leukemia. CBP has also been associated with Amyotrophic lateral sclerosis (ALS), a neurodegenerative disease with progressive degeneration of motor neurons in the brain and spinal cord, Alzheimer's disease and polyglutamine diseases such as Spinal and Bulbar Muscular Atrophy and Huntington’s disease.

How to Use:

• In vitro: SGC-CBP30 was used at 1-10 µM final concentration in various in vitro assays.
• In vivo: n/a

Reference:

1. 1. Developed by Structural Genomics Consortium (SGC) http://www.thesgc.org/

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