MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 ( MDM2 ) degrader based on the proteolysistargeting chimera ( PROTAC ) concept. MD-224 consists of ligands for Cereblon and MDM2 . MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC 50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent. MD-224 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. (Pink: MDM-2/p53 ligand ( HY-125858 ); Blue: Cereblon ligand ( HY-43722 ); Black: linker).
Products | Products > Disease Areas > Leukemia/Lymphoma/Myeloma | Products > Disease Areas > Blood Disease | Products > Disease Areas > Cancer | Products > Disease Areas > Blood or Cardio-cerebrovascular Disease | Products > Signaling Pathways > PROTAC | Products > Signaling Pathways > Metabolic Enzyme/Protease | Products > Signaling Pathways > Apoptosis | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Signaling Pathways > PROTACs | Products > Signaling Pathways > E1/E2/E3 Enzyme | Products > Signaling Pathways > MDM-2/p53
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