MYCi975

MYCi975 (CAS No.: 2289691-01-4) is a synthetically derived small-molecule research tool classified as a protein–protein interaction modulator, specifically used to intervene in the MYC transcriptional network and target the MYC:MAX dimer for biomedical research scenarios such as transcription factor biology and oncology target validation; it has also been reported under the alias NUCC-0200975. Existing mechanistic studies show that this compound can directly bind MYC and disrupt MYC:MAX complex formation, while enhancing GSK3β-dependent phosphorylation of MYC at the T58 site, thereby promoting MYC turnover via the canonical ubiquitin-coupled degradation axis and inhibiting MYC-driven gene expression programs. In vitro characterization indicates that its affinity and cellular-level activity are in the low micromolar range, with decreased viability observed in MYC-dependent prostate-derived cell models and apoptosis induced at similar concentrations in multiple breast-derived cell lines; intracellular target engagement has been supported by biophysical and chemoproteomic approaches such as cellular thermal shift assay (CETSA) and affinity capture with biotinylated analogs. In terms of mechanism-based in vivo studies, this compound has been used in MYC-driven xenograft mouse models for target validation and pathway functional studies, and oral dosing data support its in vivo pharmacological application in rodent models; all such uses are limited to basic and translational research. Typical experimental applications include perturbing MYC-dependent signaling, assessing transcriptional and phenotypic readouts, and early-stage drug discovery screening in diverse cellular and animal systems; the specific concentrations or doses used typically require empirical optimization according to the respective experimental system and research objective.