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DYRK

DYRK inhibitors act on dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs) in cell growth. The first family member, Dyrk, was described in 1996 as a kinase whose activity depends on tyrosine residues in its activation loop. DYRK1A lies in the Down syndrome critical region of chromosome 21, and DYRK1B is studied in cell quiescence. The beta-carboline alkaloid harmine inhibits DYRK1A, as shown in a 2007 kinase selectivity screen. AZ191 preferentially inhibits DYRK1B, LDN-192960 targets DYRK2, and GSK-626616 is listed as a DYRK3 inhibitor. The set also contains inhibitors of related targets such as homeodomain-interacting protein kinase 2 (HIPK2) and mitotic kinesin-like protein 2 (MKLP-2).

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  • PROTAC DYRK2 degrader 1
    Cat. No.
    A84593
    CAS No.
    3061366-76-2

    PROTAC DYRK2 degrader 1

    PROTAC DYRK2 degrader 1 is a selective degrader targeting DYRK2, functioning through the ubiquitin-proteasome system. It exhibits DC50 values of 1.607 μM in MDA-MB-231 cells and 3.265 μM in HeLa cells, effectively inducing DYRK2 degradation. This compound is valuable for research focused on triple-negative breast cancer and cervical cancer, facilitating the exploration of targeted protein degradation mechanisms in these malignancies.

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