skp2 e3 ligase

SMIP004 is an SKP2 E3 ligase inhibitor. SMIP004 is a cancer cell-selective apoptosis inducer of human prostate cancer cells.

Ubiquitination-IN-1 is an inhibitor of ubiquitination and Cksl-Skp2 protein-protein interaction (IC50: 0.17 μM).

XMU-MP-8 (SKPer1) is a potent molecular glue degrader that targets the oncogenic protein SKP2. It interacts with the F-box domain of SKP2 (Kd≈ 36 μM) and the N-terminal TPR domain of the E3 ligase STUB1 (Kd≈ 2.5 μM), leading to the formation of a stable SKP2-SKPer1-STUB1 ternary complex (Kd≈ 8.9 nM). This interaction triggers the ubiquitination and proteasomal degradation of SKP2. XMU-MP-8 selectively eradicates cancer cells expressing SKP2 and exhibits notable tumor-suppressive effects in vivo along with a favorable safety profile. It is applicable in research on cancers such as non-small cell lung adenocarcinoma (NSCLC) and prostate adenocarcinoma.

SZL P1-41, a skp2 inhibitor, can prevent assembly of Skp2-Skp1 complexes. It selectively suppresses Skp2 SCF E3 ligase activity but exhibits no effect on the activity of other SCF complexes. It also inhibits Skp2-mediated p27 and Akt ubiquitination in vivo and in vitro. It suppresses the survival of Y cells and Y stem cells by triggering cell senescence and inhibiting glycolysis. It exhibits antitumor effects in multiple animal models and Y cell lines.

Skp2 Inhibitor C1 (SKPin C1)(SKPin C1) is a specific small molecule inhibitor of Skp2-mediated p27 degradation.

p27 Analogue CP2 is a macrocyclic peptide inhibitor that targets the SCFSkp2/Cks1 E3 ubiquitin ligase complex (Kd=32 nM). By preventing the ubiquitination and subsequent degradation of the p27 protein mediated by SCFSkp2/Cks1, it helps restore p27 levels and inhibits cell proliferation. This compound shows potential for research on cancers that rely on Skp2 overexpression, such as breast cancer.