PIK-75

PIK-75 is a synthetic small molecule inhibitor that selectively targets the p110α isoform of phosphoinositide 3-kinase (PI3K), with additional activity against p110γ and DNA-dependent protein kinase (DNA-PK). It acts as a potent PI3K inhibitor with an IC50 of approximately 5.8 nM for p110α and also inhibits DNA-PK at low nanomolar concentrations. Mechanistically, it blocks PI3K/AKT signaling pathways and has been shown to induce apoptosis in cancer cells by disrupting survival signals such as MCL-1 expression and AKT activation. In preclinical studies, PIK-75 has demonstrated efficacy in overcoming resistance to venetoclax in mantle cell lymphoma models by targeting both PI3K and cyclin-dependent kinase 9 (CDK9), leading to reduced tumor cell viability even in resistant settings[1][6][8]. The compound is considered experimental and is primarily used as a research tool for studying PI3K pathway inhibition.

Other names

Benzenesulfonic acid, 2-methyl-5-nitro-, 2-((6-bromoimidazo(1,2-a)pyridin-3-yl)methylene)-1-methylhydrazide