Domatinostat

Domatinostat (CAS No.: 910462-43-0) is a synthetic small-molecule, benzamide-type epigenetic modulator, also known as 4SC-202. It is primarily classified as a selective class I histone deacetylase (HDAC) inhibitor, selectively acting on HDAC1, HDAC2, and HDAC3, and also exhibits inhibitory activity against lysine-specific demethylase 1 (LSD1); by attenuating deacetylase and demethylase functions, this compound increases histone acetylation and modulates histone methylation status, thereby promoting a more open chromatin state and reshaping transcriptional programs, associated with key biological processes such as cell-cycle progression, differentiation, DNA damage response, and immune signaling. Research focuses include chromatin regulation and transcriptional control, and it is widely used in epigenetics research in oncology and immunology model systems. In vitro, its targeting of class I HDACs is typically in the submicromolar to low micromolar range and is accompanied by detectable activity against LSD1, making it suitable as a dual epigenetic probe for mechanistic elucidation and screening workflows; typical applications include modulating epigenetic states in human- or mouse-derived cell culture models, evaluating the accumulation of acetylated histones, conducting pathway and transcriptomic profiling analyses, and incorporating it into phenotype- or target-oriented drug discovery assays and high-content screening; in animal models or complex co-culture systems, it can also be used to validate and extend epigenetic regulatory effects, while the concentrations and treatment durations used in experiments generally depend on the specific research objectives, biological system, and detection methods, and should be explored and optimized to ensure the reproducibility and interpretability of results.