SRPIN340

SRPIN340 is a small molecule inhibitor of serine/arginine-rich protein-specific kinases 1 and 2 (SRPK1 and SRPK2). These kinases are essential regulators of alternative mRNA splicing, as they phosphorylate SR proteins that select splice sites in pre-mRNA. By inhibiting SRPK1/2, SRPIN340 modulates the splicing of various genes involved in disease progression. In oncology, it has been shown to reverse the aberrant splicing of PIK3CD, thereby reducing the expression of the oncogenic PI3Kδ-S variant and sensitizing tumor cells to PI3K inhibitors like idelalisib. Beyond cancer, SRPIN340 has demonstrated potential in inhibiting the replication of various viruses, including HIV and HCV, by interfering with the splicing of viral RNA. It has also been investigated for its ability to shift VEGF splicing toward anti-angiogenic isoforms, suggesting potential utility in treating age-related macular degeneration.

Other names

N-(2-(piperidin-1-yl)-5-(trifluoromethyl)phenyl)isonicotinamide