PI-3065 (CAS: 955977-50-1) is a novel potent and selective PI3K p110δ inhibitor with IC50 of 15 nM; exhibits > 100 fold selectivity against p110α, p110β, p110γ, DNA-PK and mTOR. As p110δ is primarily expressed in leukocytes, drugs against p110δ have not been considered for the treatment of solid tumours. p110δ inactivation in regulatory T cells unleashes CD8(+) cytotoxic T cells and induces tumour regression. p110δ inhibitors can break tumour-induced immune tolerance and should be considered for wider use in oncology.
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TGF-beta/Smad
PTEN
