INK1048

INK1048 is a potent and selective small molecule inhibitor of the delta (δ) and gamma (γ) isoforms of phosphoinositide 3-kinase (PI3K), with IC50 values reported below 10 nM for both targets. Developed by Intellikine, the compound was designed to target the PI3K/mTOR signaling pathway, which is frequently dysregulated in hematological malignancies. Preclinical studies presented at the AACR 2010 meeting demonstrated that INK1048 possesses anti-proliferative activity in various B-cell malignancy models, including mantle cell lymphoma, follicular lymphoma, chronic lymphocytic leukemia (CLL), and multiple myeloma. While it effectively inhibits cell proliferation, its impact on cell viability is generally observed only at higher concentrations, characterizing it primarily as a cytostatic agent in these contexts.