PROTAC DYRK2 degrader-2 is a PROTAC DYRK2 degrader based on curcumin analog A3. It recruits the CRBN E3 ligase to mediate DYRK2 ubiquitination and achieves degradation via the ubiquitin-proteasome system. PROTAC DYRK2 degrader-2 downregulates the expression level of DYRK2 protein in cancer cells. It is applicable to cancer-related research [1]. (Pink: DYRK2 ligand; Blue: Cereblon ligand; Black: linker ).
In Vitro, PROTAC DYRK2 degrader-2 (CP124) (5-10 μM; 24 h) reduces the DYRK2 protein abundance in HeLa cervical cancer cells, and its degradation activity is weaker than that of CP134, a compound from the same series[1].
References:
[1]. Chen J, et al. Discovery of the First Potent DYRK2 Proteolysis Targeting Chimera Degraders. ACS medicinal chemistry letters. 2024 May 09;15(5):659-666.
In Vitro, PROTAC DYRK2 degrader-2 (CP124) (5-10 μM; 24 h) reduces the DYRK2 protein abundance in HeLa cervical cancer cells, and its degradation activity is weaker than that of CP134, a compound from the same series[1].
References:
[1]. Chen J, et al. Discovery of the First Potent DYRK2 Proteolysis Targeting Chimera Degraders. ACS medicinal chemistry letters. 2024 May 09;15(5):659-666.