PI 3-Kγ Inhibitor

A cell-permeable thiazolidinedione compound that acts as a potent, selective, and ATP-competitive inhibitor of phosphatidylinositol 3-kinase γ (PI 3-Kγ) (K_i = 7.8 nM; IC₅₀ = 8 nM, 60 nM, 270 nM, 300 nM for p110-γ, α, β and δ-isoforms, respectively). Does not affect the activity of a wide panel of kinases, receptors, enzymes, and ion channels even at concentrations as high as 1 µM. Selectively blocks MCP-1-, but not CSF-1-, dependent Akt phosphorylation and chemotaxis in primary Pik3cg^+/+ murine monocytes and in a human monocytic cell line THP-1 (IC₅₀ = 181 nM). Also shown to exhibit in vivo efficacy in reducing neutrophil chemotaxis in murine peritonitis and arthritis models.

A cell-permeable, potent, selective, and ATP-competitive inhibitor of phosphatidylinositol 3-kinase γ (PI 3-Kγ) (K_i = 7.8 nM; IC₅₀ = 8 nM, 60 nM, 270 nM, 300 nM for p110-γ, α, β and δ-isoforms, respectively). Does not affect the activity of a wide panel of kinases, receptors, enzymes, and ion channels even at concentrations as high as 1 µM. Selectively blocks MCP-1-, but not CSF-1-, dependent Akt phosphorylation and chemotaxis in primary Pik3cg^+/+ murine monocytes and in a human monocytic cell line THP-1 (IC₅₀ = 181 nM). Also shown to exhibit in vivo efficacy in reducing neutrophil chemotaxis in murine peritonitis and arthritis models.

Cell permeable: yes

Primary Target
Phosphatidylinositol 3-kinase γ (PI 3-Kγ)

Product competes with ATP.

Reversible: no

Target IC₅₀: 8 nM, 60 nM, 270 nM, 300 nM for p110-γ, α, β and δ-isoforms, respectively; 181 nM in selectively blocking MCP-1-, but not CSF-1-, dependent Akt phosphorylation and chemotaxis in primary Pik3cg+/+ murine monocytes and in a human mono

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Barber, D.F., et al. 2005. Nat. Med.11, 933.
Camps, M., et al. 2005. Nat. Med.11, 936.

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