Rogocekib

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable inhibitor of CLK family kinases, with potential antineoplastic activity. Upon oral administration, rogocekib binds to and inhibits the activity of CLK family kinases, thereby inhibiting the phosphorylation of serine/arginine-rich (SR) domain-containing splicing factors (SFs). This modulates RNA splicing, prevents the expression of certain tumor-associated genes, and inhibits tumor cell proliferation. In many cancer cells, core spliceosome proteins, including SF3B1, U2 small nuclear ribonucleoprotein auxiliary factor 1 (U2AF1), serine/arginine-rich splicing factor 2 (SRSF2) and U2 small nuclear ribonucleoprotein auxiliary factor subunit-related protein 2 (ZRSR2), are mutated and aberrantly activated leading to a dysregulation of mRNA splicing. CLK family kinases, an evolutionarily conserved group of kinases, phosphorylates various SR proteins including SR domain-containing SFs.

**Synonyms:** - CLK Inhibitor CTX-712 - CTX 712 - CTX-712 - CTX712 - ROGOCEKIB - Splicing Modulator CTX-712