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.
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.
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