TR-412

TR-412 is a novel, highly selective small molecule inhibitor targeting CDC2-like kinases 2 and 3 (CLK2/3) and dual-specificity tyrosine-regulated kinases 1A and 1B (DYRK1A/B). Developed by Tarapeutics Pharmaceutical Science, it is designed to modulate alternative splicing, a process frequently dysregulated in cancer. By inhibiting the phosphorylation of serine/arginine-rich splicing factors (SRSFs), TR-412 induces global splicing changes, specifically exon skipping, which leads to anti-proliferative effects in hematological malignancies. Preclinical studies in acute myeloid leukemia (AML) models have demonstrated significant tumor growth suppression and complete regression in MV4-11 xenograft models.