Cirtuvivint

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable small molecule ATP-competitive inhibitor of CDC2-like kinase (CLK) and dual specificity tyrosine-phosphorylation-regulated kinase (DYRK) family kinases, with potential antineoplastic activity. Upon oral administration, cirtuvivint targets, binds to and inhibits the activity of CLK and DYRK family of protein kinases, including CLK1-4 and DYRK1-4, thereby inhibiting the phosphorylation of serine/arginine-rich (SR) domain-containing splicing factors (SFs). This modulates RNA splicing and inhibits the expression of genes involved in the Wnt signaling pathway. This decreased expression of Wnt pathway-related genes prevents Wnt signaling and may inhibit proliferation of cancer cells in which the Wnt signaling pathway is overactivated. The Wnt signaling pathway is dysregulated in many cancer cell types and plays a crucial role in tumor cell proliferation. CLK and DYRK family kinases, evolutionarily conserved groups of dual specificity kinases, phosphorylate various SR proteins including SR domain-containing SFs.

**Synonyms:** - CIRTUVIVINT - SM 08502 - SM-08502 - SM08502 - Wnt Signaling Pathway Inhibitor SM08502