KS-20260

KS-20260 is a potent small molecule inhibitor of Iron Regulatory Protein 2 (IRP2), developed by AIGEN Sciences using their AI-driven AIGEN InSight platform. IRP2 is a key regulator of intracellular iron homeostasis and is frequently overexpressed in colorectal cancer (CRC), where it contributes to tumor progression. KS-20260 was optimized from earlier IRP2 inhibitors to provide enhanced potency. Research indicates that KS-20260 exhibits synergistic antitumor efficacy when combined with the EGFR inhibitor osimertinib in CRC models. This combination therapy disrupts cell-cycle progression by downregulating key regulators such as CDK1, AURKB, CENPF, and E2F8, leading to significant reductions in tumor volume and weight in vivo.