DYRK

FINDY is a selective inhibitor of DYRK1A, specifically targeting its folding intermediate. It effectively inhibits autophosphorylation at Ser97, with an IC50 of 35 μM. FINDY is valuable for research on neurological disorders. Additionally, it features an alkyne group that allows it to engage in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a versatile tool in chemical biology applications.

Norharmine is a Harmine analogue that functions as an inhibitor of monoamine oxidase A (MAO-A) and dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A). It exhibits weak inhibitory activity against MAO-A and demonstrates certain inhibitory effects on DYRK1A, positioning it as a valuable tool for research in neurobiology and cellular signaling pathways. Norharmine is useful in studies focusing on mood disorders and cognitive functions related to these kinase targets.

Dyrk1A-IN-11 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), exhibiting an EC50 of 0.0021 µM. This compound effectively inhibits the phosphorylation of Tau at threonine 212, with an EC50 value of 0.0361 µM. Dyrk1A-IN-11 is relevant for research into neurodegenerative diseases and the role of tau phosphorylation in cellular processes.

Aristolactam BIII is a selective inhibitor of DYRK1A, demonstrating potent inhibition of the kinase's activity in vitro with an IC50 of 9.67 nM. This compound effectively rescues proliferative defects in DYRK1A transgenic mouse-derived fibroblasts and ameliorates neurological and phenotypic abnormalities in Down syndrome-like Drosophila models. Its applications are valuable in studying the role of DYRK1A in various biological processes and diseases, particularly in the context of developmental disorders.

DYRKi is a selective inhibitor of DYRK1 and DYRK1B, exhibiting IC50 values of 3.7 µM and 90 nM, respectively. This compound effectively antagonizes Hh/Gli signaling pathways, disrupting both SMO-dependent and SMO-independent oncogenic GLI activity in human medulloblastoma cells. DYRKi holds potential for research focused on HH/GLI-associated cancers, providing a valuable tool for elucidating the role of these pathways in tumorigenesis.

ProINDY is a prodrug of INDY that functions as an inhibitor of DYRK1A and DYRK1B. This compound has demonstrated the ability to recover Xenopus embryos from head malformations caused by the overexpression of Dyrk1A. ProINDY is valuable for research applications related to developmental biology and the study of kinase pathways involved in embryogenesis.

Dyrk1A-IN-2 is a potent DYRK1A inhibitor with an EC50 of 37 nM. This compound demonstrates significant capacity to promote human β-cell replication while exhibiting low cytotoxicity. Dyrk1A-IN-2 is a valuable tool for research in diabetes and regenerative medicine, aiding in the investigation of β-cell proliferation and function.

Dyrk1A-IN-12 is a selective inhibitor of Dual specificity tyrosine phosphorylation regulated kinase 1A (Dyrk1A), demonstrating an IC50 of 95 nM. This compound exhibits significant anti-Enterovirus A71 (EV-A71) activity, with an EC50 of 4.4 μM and a cytotoxicity CC50 of 12.8 μM, resulting in a selectivity index of 2.9. Additionally, Dyrk1A-IN-12 shows strong inhibitory effects against herpes simplex virus (HSV), positioning it as a valuable tool for research in viral infections and Dyrk1A-related pathways.

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.