Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Primary TargetPI 3-Kα

Target IC₅₀: 2 nM, 16 nM, 660 nM, and 220 nM for p110α, p110β p110γ, and PI 3-K C2β, respectively

Cell permeable: yes

General description

A cell-permeable morpholino-thienopyrimidine compound that acts as a potent and isoform-selective inhibitor of PI 3-Ks (IC_{50﹤/sub> = 2 nM, 16 nM, 660 nM, and 220 nM for p110A, p110β p110γ, and PI 3-K C2β, respectively) and inhibits non-PI 3-K kinases only at much higher concentrations (IC50﹤/sub> ≥ 3.4 µM for Cdk2/E, KDR, PKA, and PKCA). Shown to inhibit cell proliferation (IC50﹤/sub> = 580 nM) and serum-stimulated Akt phosphorylation (IC50﹤/sub><3 µM) in A375 melanoma cells.}

A cell-permeable morpholino-thienopyrimidine compound that acts as a potent and isoform-selective inhibitor of PI 3-kinases (IC_{50﹤/sub> = 2 nM, 16 nM, 660 nM, and 220 nM for p110A, p110β p110γ, and PI 3-K C2β, respectively) and inhibits non-PI 3-K kinases only at much higher concentrations (IC50﹤/sub> ≥3.4 µM for Cdk2/E, KDR, PKA, and PKCA). Shown to inhibit cell proliferation (IC50﹤/sub> = 580 nM) and serum-stimulated Akt phosphorylation (IC50﹤/sub><3 µM) in A375 melanoma cells.}

Legal Information

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

Other Notes

Hayakawa, M., et al. 2006. Bioorg. Med. Chem.14, 6847.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Reconstitution

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

Warning

Toxicity: Irritant (B)