RG7112D is a potent MDM2 inhibitor with IC 50 s of 11 nM and >10000 nM and for MDM2-p53 and VHL-HIF1α by binding HTRF assay, respectively. RG7112D is coupled by an amide bond to VHL-Amine, resulting in a bi-functional molecule, YX-02-030. YX-02-03, a MDM2-PROTAC, potently inhibits MDM2-p53 binding (HTRF IC 50 =63nM). RG7112D can stabilize MDM2 protein and increase p53 protein levels.