PI 3-K inhibitor IX, PIK-90

Toxicity: Standard Handling (A)

A cell-permeable imidazoquinazoline compound that acts as a potent, reversible, and ATP-competitive inhibitor against all three classes of PI 3-K kinases (IC₅₀ = 11, 18, 47, 58, 64, 350, and 830 nM against p110α, p110γ, PI 3-KC2α, p110δ, PI 3-KC2β, p110β, and hsVPS34, respectively), as well as several PIKKs (IC₅₀ = 13, 610, and 1050 nM against DNA-PK, ATM, and mTORC1, respectively) and PI 4-KIIIα (IC₅₀ = 830 nM), while exhibiting much reduced potency against PI 4-KIIIβ and ATR (IC₅₀ = 3.1 and 15 µM, respectively) and little or no activity toward PI 4-KIIα, PIPKs (IC₅₀ >100 µM), and a panel of 36 commonly studied protein kinases (<15% inhibition at 10 µM). Effectively suppreses insulin-stimulated phosphorylations of Akt and rpS6 in 3T3-L1 adipocytes and L6 myotubes in a dose-dependent manner in vitro (by >90% at 2.5 µM) and completely prevents insulin-induced blood glucose decline in mice in vivo (10 mg/ml, i.p.).

Fan, Q.W., et al. 2007. Cancer Res.67, 7960.
Fan, Q.W., et al. 2006. Cancer Cell9, 341.
Knight, Z.A., et al. 2006. Cell125, 733.

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Slight warming may be required to for complete solubility.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany