MRT5413

MRT5413 is a potent and selective molecular glue degrader (MGD) targeting cyclin-dependent kinase 2 (CDK2), developed by Monte Rosa Therapeutics. CDK2 is a key regulator of the cell cycle, particularly the G1/S transition, and its dysregulation is implicated in various cancers, including breast and ovarian cancers, often as a mechanism of resistance to CDK4/6 inhibitors. MRT5413 functions by facilitating the interaction between CDK2 and the Cereblon (CRBN) E3 ubiquitin ligase complex, leading to the polyubiquitination and subsequent proteasomal degradation of CDK2. By eliminating the CDK2 protein rather than just inhibiting its kinase activity, MRT5413 aims to overcome the compensatory mechanisms and scaffolding functions that often limit the efficacy of traditional small-molecule inhibitors.