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-HIF1alpha 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[1].
Molecular Weight:
1267.41
Purity:
99.86
CAS Number:
[3049076-98-1]
Formula:
C66H85Cl2N9O10S
Target:
Apoptosis,MDM-2/p53,PROTACs
Application Notes:
MCE Product type: Reference compound
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