HM5023507 is a potemt, selective, orally active dual PI3Kδ/γ inhibitor with IC50 of 4 nM and 5 nM for p110γ and p110δ, respectively.
HM5023507 displays 100‐fold selectivity against PI3Kα and PI3Kβ in recombinant enzymatic assays and in primary human immune cells with an exquisite selectivity against other targets.
HM5023507 attenuated anti‐CD3/anti‐CD28‐induced human T cell activation, with a better potency in the blockade of IL‐2 production than in proliferation response, with IC50 values of 9 and 120 nM, respectively.
HM5023507 reduces T cell differentiation into different effector cell types including Th1, Th2, Th17, and Treg cells with mean IC50 values of 48, 18, 63, and 130 nM, respectively.
HM5023507 inhibited anti‐IgM‐induced activation as measured by upregulation of CD69 and IL‐6 production from purified human B cells (IC50<10 nM), also attenuated B cell activation in rat whole blood with an average IC50 of 44 nM.
HM5023507 (3 mg/kg, p.o.) attenuates B cell activation and CXCL1 induced neutrophil influx in female Wistar rats.