General description
A cell-permeable morpholino-thienopyrimidine compound that acts as a potent and isoform-selective inhibitor of PI 3-Ks (IC50 = 2 nM, 16 nM, 660 nM, and 220 nM for p110α, p110β p110γ, and PI 3-K C2β, respectively) and inhibits non-PI 3-K kinases only at much higher concentrations (IC50 ≥ 3.4 µM for Cdk2/E, KDR, PKA, and PKCα). Shown to inhibit cell proliferation (IC50 = 580 nM) and serum-stimulated Akt phosphorylation (IC50<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 (IC50 = 2 nM, 16 nM, 660 nM, and 220 nM for p110α, p110β p110γ, and PI 3-K C2β, respectively) and inhibits non-PI 3-K kinases only at much higher concentrations (IC50 ≥3.4 µM for Cdk2/E, KDR, PKA, and PKCα). Shown to inhibit cell proliferation (IC50 = 580 nM) and serum-stimulated Akt phosphorylation (IC50<3 µM) in A375 melanoma cells.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
PI 3-Kα
Product does not compete with ATP.
Reversible: no
Target IC50: 2 nM, 16 nM, 660 nM, and 220 nM for p110α, p110β p110γ, and PI 3-K C2β, respectively
Packaging
Packaged under inert gas
Warning
Toxicity: Irritant (B)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Hayakawa, M., et al. 2006. Bioorg. Med. Chem.14, 6847.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 41116113
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 528111-5MG