The bromodomain and PHD finger-containing (BRPF) proteins are scaffolding components of chromatin-binding MOZ/MORF histone acetyltransferase complexes, which have activity as transcriptional regulators. BRPF1 (BR140 or Peregrin) is important for maintaining Hox gene expression and the development of multiple tissues, axial skeleton, and the hematopoietic system. NI-57 is a potent inhibitor of the bromodomains of BRPF proteins that binds to BRPF1B, BRPF2, and BRPF3 with Kd values of 31, 108, and 408 nM, respectively, as determined by isothermal titration calorimetry. It is selective for BRPFs over other bromodomains. NI-57 shows accelerated FRAP recovery at 1 μM in the BRPF2 FRAP assay, preventing binding of full-length BRPF2 to chromatin. See the Structural Genomics Consortium (SGC) website for more information.
The bromodomain and PHD finger-containing (BRPF) proteins are scaffolding components of chromatin-binding MOZ/MORF histone acetyltransferase complexes, which have activity as transcriptional regulators. BRPF1 (BR140 or Peregrin) is important for maintaining Hox gene expression and the development of multiple tissues, axial skeleton, and the hematopoietic system.
NI-57 has favorable oral bioavailability in mice[1].
[1]. http://www.thesgc.org/chemical-probes/ni-57
[2]. klein bj, lalonde me, cté j, et al. crosstalk between epigenetic readers regulates the moz/morf hat complexes. epigenetics. 2014 feb;9(2):186-93.
[3]. ullah m, pelletier n, xiao l, et al. molecular architecture of quartet moz/morf histone acetyltransferase complexes. mol cell biol. 2008 nov;28(22):6828-43.
