tcsc0582 NVP-BAG956

NVP-BAG956 is an ATP-competitive PI3K inhibitor with IC50s of 34, 56, 112 and 444 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.

IC50 & Target: IC50: 34 nM (PI3Kδ), 56 nM (PI3Kα), 112 nM (PI3Kγ), 444 nM (PI3Kβ), 240/260 nM (PDK1)^[1]

In Vitro: NVP-BAG956 also inhibits PDK1 with an IC₅₀ of 240/260 nM. NVP-BAG956 also inhibits VEGFR1 with an IC₅₀ of 2.56±0.56 μM. NVP-BAG956 blocks phosphorylation of PKB/Akt in A2058 cells with an IC₅₀ value of 67±25 nM. Inhibition of PKB/Akt phosphorylation correlated with loss of A2058 cell proliferation for NVP-BAG956 (IC₅₀=290±20 nM). In the presence of NVP-BAG956, A2058 cells are only able to exit G2-M and then remain in G1. The p27 ^Kip1 expression is clearly induced by NVP-BAG956 in A2058 cells but not in C32 cells^[1].