PIK-75

The Uses of PIK-75

PIK-75 is a p110α inhibitor, isoform-specific mutants at Ser773, and also potently inhibits DNA-PK.

What are the applications of Application

PIK-75, free base is a free base is a selective inhibitor of PI 3-kinase p110α

Definition

ChEBI: N-[(6-bromo-3-imidazo[1,2-a]pyridinyl)methylideneamino]-N,2-dimethyl-5-nitrobenzenesulfonamide is a sulfonamide.

Enzyme inhibitor

This novel phosphoinositide-3 kinase p110α inhibitor (F.Wt. = 488.74; CAS 372196-67-3; Solubility (25°C): 98 mg/mL DMSO, <1 mg/mL Water), also known as (E)-N'-((6-bromoH-imidazo[1,2-a]pyridin-3-yl)methylene)-N,2- dimethyl-5-nitrobenzenesulfonohydrazide-HCl, competes with respect to a substrate (phosphatidylinositol, PI), unlike most other PI3K inhibitors, which bind at or near the ATP site. PIK-75 exhibits impressive isoform selectivity, with an IC50 value of 5.8 nM for p110α, while the corresponding IC50 values are 1300 nM, 76 nM and 510 nM for p110β, p110γ, and p110δ, respectively.