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IPI-3063 is a potent and selective PI3K p110δ inhibitor with an IC50 of 2.5 ± 1.2 nM.

IPI-3063 inhibits p110α, p110β, and p110γ with IC50s of 1171±533 nM, 1508±624 nM, and 2187±1529 nM, respectively. IPI-3063 potently reduces mouse B cell proliferation, survival, and plasmablast differentiation while increasing antibody class switching to IgG1. IPI-3063 is a p110δ selective compound with an IC50=0.1 nM in p110δ-specific cell-based assays and cellular IC50 values for the other class I PI3K isoforms are at least 1,000-fold higher (IC50=1901±1318 nM for p110α, IC50=102.8±35.7 nM for p110β, IC50=418.8±117.2 nM for p110γ). IPI-3063 is very potent in reducing p-AKT (significant effect at 1 nM). IPI-3063 also reduces p-ERK1/2 with a significant effect at 10 nM. IPI-3063 is very potent, achieving a significant decrease in B cell survival when present at 10 nM[1].

[1]. Chiu H, et al. The Selective Phosphoinoside-3-Kinase p110δ Inhibitor IPI-3063 Potently Suppresses B Cell Survival, Proliferation, and Differentiation. Front Immunol. 2017 Jun 30;8:747.

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