Silmitasertib is a potent and orally bioavailable inhibitor of casein kinase 2 (Ki=0.38 nM) acting at the ATP-binding site.1 It has been in preclinical and clinical development for a variety of cancers.2 It inhibits CK2-mediated phosphorylation of the SALL2 tumor suppressor preventing its proteasomal degradation and induces cell death in a variety of tumor cell lines.3 It inhibits fibroblast-like synoviocytes reducing rheumatoid arthritis disease severity in rodent models4 and inhibits collagen degradation5.
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