Polo-like Kinase (PLK) Degrader

MDEG-541 is a PROTAC degrader targeting MYC, GSPT1/2 and PLK1. MDEG-541 induces degradation via proteasome- and ubiquitin-dependent pathways. MDEG-541 exhibits anti-tumor activity in gastrointestinal cancer cells and patient-derived organoids. MDEG-541 can be used for the research of gastrointestinal cancer.

SP27 is a PROTAC PLK4 degrader with an IC₅₀ of 8.4 nM and a DC₅₀ of 19.5 nM against PLK4. SP27 induces PLK4 degradation via the CRBN-dependent ubiquitin-proteasome pathway, inhibits PLK4 downstream signal transduction, and suppresses the growth of TRIM37-amplified breast cancer cells. SP27 is applicable for breast cancer-related research.

PROTAC PLK1 Degrader-2 is a peptide-based N-end rule PLK1 mini-PROTAC. PROTAC PLK1 Degrader-2 utilizes Arg12 as dual-function cell-permeable N-degron to recruit UBR1/UBR2 E3 ligases, mediates PLK1 ubiquitination and proteasome-dependent degradation. PROTAC PLK1 Degrader-2 suppresses cervical cancer cell proliferation, induces G2/M cell cycle arrest and tumor cell apoptosis, and exerts potent in vivo anti-tumor efficacy in mice and can be applied to research on PLK1-driven cervical carcinoma.

PROTAC PLK1 Degrader-3 (Compound DD-1) is a PLK1 PROTAC degrader based on the N-deglycosylation pathway, with a K_d value of 2.2 μM. The cell penetration ability of PROTAC PLK1 Degrader-3 is limited and a higher concentration is required to achieve significant degradation effects. PROTAC PLK1 Degrader-3 can be used for research on non-small cell lung cancer.

L14-8 is a potent ferroptosis inducer. L14-8 promotes PLK1 degradation via ubiquitination, increasing TP53 phosphorylation to enhance SAT1 transcription, thereby triggering ferroptosis and cancer cell death. L14-8 can be used for the study of advanced prostate cancer.

POI ligand-4 is a PLK1 ligand and can be used for the synthesis of PROTACs, such as PROTAC PLK1 Degrader-3 (HY-181000).