Asawa, Rosita R. published the artcileA Comparative Study of Target Engagement Assays for HDAC1 Inhibitor Profiling, Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, the main research area is cancer neurodegeneration HDAC1 NanoBRET SplitLuc CETSA; HDAC1; NanoBRET; SplitLuc CETSA; epigenetic compound library; profiling; qHTS; target engagement.
Histone deacetylases (HDACs) are epigenetic modulators linked to diseases including cancer and neurodegeneration. Given their therapeutic potential, highly sensitive biochem. and cell-based profiling technologies have been developed to discover small-mol. HDAC inhibitors. Ultimately, the therapeutic action of these inhibitors is dependent on a phys. engagement with their intended targets in cellular and tissue environments. Confirming target engagement in the cellular environment is particularly relevant for HDACs since they function as part of cell type-specific multiprotein complexes. Here we implemented two recently developed high-throughput target engagement technologies, NanoBRET and SplitLuc CETSA, to profile 349 compounds in the Epigenetic-Focused collection for HDAC1 binding. We found that the two HDAC1 target engagement assays correlated well with each other and with orthogonal activity-based assays, in particular those carried out in cellular environments rather than with isolated HDAC proteins. The assays detected a majority of the previously described HDAC1 inhibitors in the collection and, importantly, triaged HDAC inhibitors known to target other HDACs.
SLAS Discovery published new progress about Cell proliferation. 55981-09-4 belongs to class esters-buliding-blocks, name is 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate, and the molecular formula is C12H9N3O5S, Name: 2-((5-Nitrothiazol-2-yl)carbamoyl)phenyl acetate.
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics