A bromodomain is an approximately 110 amino acid protein domain that recognizes monoacetylated lysine residues such as those on the N-terminal tails of histones. Members of the BET family (Bromodomain and extra terminal domain family) have been implicated as targets in human cancer. SGC has developed an inhibitor, I-CBP112, against the CREBBP and EP300 Bromodomains (IC50: 170 nm (CREBBP/EP300)).

In vitro: A CREBBP/EP300-selective chemical probe from a completely different structural class which was also developed by the SGC is I-CBP112. I-CBP112 has an IC50 value of 170 nm in the CREBBP AlphaScreen assay and is selective against the bromodomain proteins ATAD2, BAZ2B, BRD2(BD2), BRD4 (BD1), PB1(BD5), PCAF, PHIP(BD2), TRIM24/TIF-1a. In U2OS cells no significant cytotoxicity up to 50 mm was found. Similar to bromosporine 129, data related to SGCCBP30 and I-CBP112 are reported on the SGC homepage exclusively [1].

In vivo: Currently, I-CBP112 is still in the in-vitro investigation, and no animal in-vivo study is on-going.

T22846

C27H36N2O5

468.59

I-CBP 112

1eq. HCl:100 mM
DMSO:100 mMmg
Powder: -20°C for 3 years
In solvent: -80°C for 2 years