compound 8430

Compound 8430 (also known as NCGC00188430) is a small molecule inhibitor designed to disrupt the protein-protein interaction between the SIX1 homeobox protein and its transcriptional co-activator EYA2. SIX1 is a developmental transcription factor that is typically silenced post-embryogenesis but is frequently reactivated in various cancers, including solid tumors and certain leukemias such as CALM-AF10-rearranged T-cell acute lymphoblastic leukemia (T-ALL) and acute myeloid leukemia (AML). By preventing the formation of the SIX1/EYA2 complex, compound 8430 inhibits the transcriptional activity of SIX1, leading to reduced cell proliferation and self-renewal in leukemia cells. Preclinical research has demonstrated that compound 8430 can synergize with CRM1 inhibitors like selinexor (KPT-330) to further impair leukemic growth, suggesting a potential novel therapeutic approach for SIX1-driven malignancies.

Other names

SIX1/EYA2 inhibitor 8430