XMU-MP-8

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].

2271314-01-1

SKPer1

12352005

H302, H315, H319, H335

E1/E2/E3 Enzyme; Molecular Glues

Metabolic Enzyme/Protease; PROTAC

Cancer-programmed cell death

Cancer

99.23

DMSO : 125 mg/mL (ultrasonic)

CN1N=CC2=C(NCC3=CC=CN=C3)N=C(C4=CC=CC(NC(NC5=CC=CC(C(F)(F)F)=C5)=S)=C4)N=C21

C26H21F3N8S

534.56

H302, H315, H319, H335

[1]Chu Y, et al. A rapid imaging-based screen for induced-proximity degraders identifies a potent degrader of oncoprotein SKP2. Nat Biotechnol. 2025 Sep 10.

Room Temperature

-20°C, 3 years; 4°C, 2 years (Powder)

http://file.medchemexpress.com/batch_PDF/HY-W1128879/XMU-MP-8-SDS-MedChemExpress.pdf

Reference compound1

No Development Reported