Description
SGC-CBP30 is a potent CBP/p300 bromodomain (BRD) inhibitor. SGC-CBP30 shows Kd values are 21 and 32 nM for CBP and p300 BRDs respectively. SGC-CBP30 also exhibits 40-fold and 250-fold selectivity for CBP over the first BRD of BRD4 (BRD4(1)) and BRD4(2) respectively. SGC-CBP30 accelerates FRAP recovery in cells at a concentration of 1 M.
Biochem/physiol Actions
SGC-CBP30 is a selective inhibitor of the bromodomain-containing transcription factors CREBBP (CBP) and EP300 (IC50 = 0.021 and 0.038 μM, respectively). SGC-CBP30 has little activity against other bromodomains at concentrations up to 1 mM. For full characterization details, please visit the SGC-CBP30 probe summary on the Structural Genomics Consortium (SGC) website.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
