rg7112

RG7112 (RO5045337) (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor.

RG7112D is a potent MDM2 inhibitor, effectively inhibiting MDM2-p53 and VHL-HIF1α interactions with IC50 values of 11 nM and >10000 nM, respectively, as determined by HTRF binding assays. It couples with VHL-Amine via an amide bond to form the bifunctional molecule YX-02-030. YX-02-030 acts as an MDM2-PROTAC, efficiently blocking MDM2-p53 binding (HTRF IC50= 63 nM). Additionally, RG7112D stabilizes MDM2 protein and enhances p53 protein levels.