YX-02-030

Overview

YX-02-030 is a VHL-dependent MDM2 PROTAC degrader with a K d 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 IC 50 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. (Pink: MDM2 ligand ( HY-158685 ); Blue: VHL ligand ( HY-125845 ); Black: linker ( HY-140189 )).

Application

Products | Products > Disease Areas > Cancer | Products > Signaling Pathways > PROTAC | Products > Signaling Pathways > Apoptosis | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Signaling Pathways > PROTACs | Products > Signaling Pathways > MDM-2/p53 | Products > Signaling Pathways > Apoptosis

Product Information

• Catalog No.: HY-158684
• CAS No.: 3049076-98-1
• Molecular Formula: C66H85Cl2N9O10S
• Molecular Weight: 1267.41
• Purity: 99.86%
• Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
• Solubility: ≥ 2.5 mg/mL (1.97 mM); Clear solution
• Availability: In-stock

Source

Original product source