XMU-MP-8 (SKPer1) is a potent molecular glue degrader that targets the oncoprotein SKP2. XMU-MP-8 simultaneously binds to the F-box domain of SKP2 (Kd ~ 36 µM) and the N-terminal TPR domain of the E3 ligase STUB1 (Kd ~ 2.5 µM), forming a stable SKP2-SKPer1-STUB1 ternary complex (Kd ~ 8.9 nM) that induces SKP2 ubiquitination and proteasomal degradation. XMU-MP-8 selectively eliminates SKP2-expressing cancer cells. XMU-MP-8 exhibits substantial tumour suppression with good safety profiles in vivo. XMU-MP-8 can be used for cancer research, such as non-small cell lung adenocarcinoma (NSCLC) and prostatic adenocarcinoma[1].
Molecular Weight:
534.56
Purity:
99.23
CAS Number:
[2271314-01-1]
Formula:
C26H21F3N8S
Target:
E1/E2/E3 Enzyme,Molecular Glues
Application Notes:
MCE Product type: Reference compound
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