Inobrodib

Inobrodib (CAS No.: 2222941-37-7) is a synthetic small-molecule epigenetic modulator classified as a bromodomain-selective inhibitor of the transcriptional coactivators p300 and CREB-binding protein CBP, suitable for exploring chromatin acetylation-dependent regulation of gene transcription and tumor transcription biology research contexts. It exhibits low-nanomolar affinity for the p300 and CBP bromodomains (Kd approximately 1.3 and 1.7 nM), with approximately hundred-fold selectivity over BRD4, which is in the hundreds of nanomolar range, consistent with a mechanism of action involving blockade of bromodomain recognition of acetylated lysine marks, thereby weakening coactivator recruitment to chromatin and transcription complex assembly. In cellular systems, Inobrodib can inhibit androgen receptor signaling and downregulate c?Myc-driven transcriptional programs, showing proliferation-inhibitory activity in the nanomolar to low micromolar range in prostate cancer- and hematologic tumor-related cell models. As a chemical probe for the p300/CBP bromodomain, it is commonly used to elucidate epigenetic dependencies, perform target validation, analyze pathway interactions with AR and Myc networks, and support phenotypic or targeted screening and mechanism-of-action studies; at the animal model level, it has also been used to evaluate the regulation of target gene expression and related phenotypes. The concentrations or doses used in experiments typically depend on the specific experimental design and research objectives. This compound is limited to laboratory research use, such as in cell and animal models, and is not intended for any form of human ingestion or medical use.