I3IN-002

I3IN-002 is a novel small molecule inhibitor of the RNA-binding protein IGF2BP3 (Insulin-like growth factor 2 mRNA-binding protein 3), an oncofetal protein that is highly expressed in various malignancies but absent in most adult tissues. Developed by researchers at the University of California, Los Angeles (UCLA), I3IN-002 was identified through a high-throughput screen using TR-FRET technology. The compound disrupts the interaction between IGF2BP3 and its target mRNAs, such as CDK6, HOXA9, and BCL2, thereby inhibiting the proliferation of leukemic cells. In preclinical studies, I3IN-002 demonstrated potent anti-leukemic activity in MLL-rearranged B-cell acute lymphoblastic leukemia (B-ALL) and acute myeloid leukemia (AML) models, showing significant reduction in leukemic burden and stem cell populations in vivo.