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ICA-1S is a novel small molecule inhibitor specifically targeting atypical Protein Kinase C-iota (PKC-ι). PKC-ι is an oncogenic protein kinase that is frequently overexpressed in various malignancies, including atypical teratoid rhabdoid tumor (ATRT), a rare and aggressive pediatric brain cancer. ICA-1S exerts its antitumor effects by intercepting key signaling cascades, specifically the PKC-ι/Cdk7/Cdk2 and PKC-ι/Bad pathways, which are critical for cell cycle regulation and survival. Preclinical studies have demonstrated that ICA-1S can significantly reduce cancer cell proliferation and survival, particularly when used in synergistic combination with the XPO1 inhibitor selinexor. The compound is primarily being investigated as a targeted therapy for pediatric CNS tumors characterized by SMARCB1 deficiencies.
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