INK1138

INK1138 is a potent and selective small molecule inhibitor of the delta (δ), gamma (γ), and beta (β) isoforms of phosphoinositide 3-kinase (PI3K), with IC50 values below 10 nM for each targeted isoform. Developed by Intellikine, the compound was designed to selectively modulate the PI3K/mTOR signaling pathway, which plays a critical role in the pathogenesis of various hematological malignancies. Preclinical data presented at the AACR 2010 Annual Meeting demonstrated that INK1138 possesses anti-proliferative and pro-apoptotic activity in B-cell malignancy models, including mantle cell lymphoma, follicular lymphoma, chronic lymphocytic leukemia, and multiple myeloma. By targeting the δ, γ, and β isoforms while sparing the α isoform, INK1138 aims to inhibit key survival signals in malignant B-cells while potentially minimizing the metabolic side effects associated with broader PI3K inhibition.