KT-253

KT-253 is a p53 stabilizer and a PROTAC degrader of MDM2 (DC50=0.4 nM) . It inhibits the proliferation of cancer cells RS4;11 with an IC50 of 0.3 nM, induces cell cycle arrest in the G2/M phase, and triggers apoptosis. In mouse models, KT-253 demonstrates antitumor activity. (Pink: ligand for target protein MDM2 ligand 4; Black: linker; Blue: ligand for E3 ligase cereblon)

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