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PIK-75 is a specific inhibitor of p110α isoform of PI3K with IC50 of 5.8 nM [1].

In acute myeloid leukemia cells, PIK-75 targeted the p110α isoform of PI3K, which led to a loss of connection between Bcl-xL and Bak. PIK-75 also transiently decreased Cdk7/9, leading to loss of Mcl-1 protein, and alleviation of its inhibition of pro-apoptotic Bak. The simultaneous loss of Bcl-xL and Mcl-1 led to rapid apoptosis. [2] In human monocyte-endothelial cell, PIK-75 suppressed the events of downstream signaling, including AKT phosphorylation, IKK activation, and NF-kB transcription. PIK-75 inhibited in vitro and in vivo production of TNF-α and IL-6, decreased the E-selectin, ICAM-1, and VCAM-1 expression, and blocked cell adhesion [3]. In human smooth muscle cells, PIK-75 decreased TNF-α-induced CD38 expression in asthmatic and nonasthmatic cells [4]. In pancreatic β-cells, acute treatment with PIK-75 enhanced the glucose-induced insulin secretion [5].

In vivo, PIK-75 significantly suppressed the histological abnormalities associated with dextran sulfate sodium-induced murine colitis. PIK-75 can attenuate experimental inflammation in the colon [3].

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