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YX-02-030

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-158684
    YX-02-030

    		PROTACs MDM-2/p53 Apoptosis Cancer
    YX-02-030 is a VHL-dependent MDM2 PROTAC degrader with a Kd of 35 nM. YX-02-030 recruits the VHL E3 ligase to form a ternary complex, leading to ubiquitination and proteasome-mediated degradation of MDM2. YX-02-030 inhibits MDM2-p53 and VHL-HIF1α binding with IC50 values of 63 and 1350 nM. YX-02-030 activates TAp73, upregulates p53 family target genes and induces apoptosis. YX-02-030 demonstrates on-target efficacy in TNBC xenograft-bearing mice, extending survival without normal cell toxicity .
    YX-02-030
  • HY-158685
    RG7112D

    		MDM-2/p53 Cancer
    RG7112D is a potent MDM2 inhibitor with IC50s 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 IC50=63nM). RG7112D can stabilize MDM2 protein and increase p53 protein levels .
    RG7112D
  • HY-158684A
    (4R,5S)-YX-02-030

    		Drug Isomer Cancer
    (4R,5S)-YX-02-030 is an isomer of YX-02-030 (HY-158684). YX-02-030 is a PROTAC MDM2 degrader .
    (4R,5S)-YX-02-030

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