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DYRKi is a novel nontoxic and selective DYRK1 inhibitor. | [Uses]
DYRKi is an inhibitor of DYRK1 and DYRK1B with IC50 values of 3.7 μM and 90 nM, respectively, which is used as a potent antagonist of Hh/Gli signaling. DYRKi impairs SMO-dependent and SMO-independent oncogenic GLI activity in human medulloblastoma cells. DYRKi is promising for research of HH/GLI-associated cancers[1]. | [References]
[1] Kokkorakis N, et al. Mirk/Dyrk1B Kinase Inhibitors in Targeted Cancer Therapy. Pharmaceutics. 2024 Apr 11;16(4):528. DOI:10.3390/pharmaceutics16040528 [2] Gruber W, et al. DYRK1B as therapeutic target in Hedgehog/GLI-dependent cancer cells with Smoothened inhibitor resistance. Oncotarget. 2016 Feb 9;7(6):7134-48. DOI:10.18632/oncotarget.6910 |
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