PI3-Kinase α Inhibitor 2

Description

PI3-Kinase α (PI3Kα) inhibitor 2 is an inhibitor of PI3K p110α (IC₅₀ = 2 nM in an enzyme assay). It is selective for p110α over p110β, p110γ, and PI3K C2β (IC₅₀s = 16, 660, and 220 nM, respectively). It also inhibits mammalian target of rapamycin (mTOR; IC₅₀ = 49 nM). PI3Kα inhibitor 2 inhibits proliferation in A375 melanoma cells with an IC₅₀ value of 0.58 μM.

Uses

PI3K-IN-18 (Compound 1) is a PI3K inhibitor, and can also effectively inhibit the homologous enzymemTOR. The IC50 values of PI3K-IN-18 for mTOR and PI3K-α were 49 nM and 41 nM, respectively[1].

Definition

ChEBI: PI3-Kinase alpha Inhibitor 2 is an organonitrogen heterocyclic compound, an organosulfur heterocyclic compound and an organic heterobicyclic compound.

IC 50

mTOR: 49 nM (IC₅₀); PI3Kα: 41 nM (IC₅₀)

References

[1] Verheijen, Jeroen C et al. “Discovery of 2-arylthieno[3,2-d]pyrimidines containing 8-oxa-3-azabi-cyclo[3.2.1]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K.” Bioorganic & medicinal chemistry letters vol. 20,1 (2010): 375-9. DOI:10.1016/j.bmcl.2009.10.075