A cell-permeable, reversible, potent, and selective inhibitor of Akt1/Akt2 activity (IC50=58nM, 210nM, and 2.12uM for Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays). The inhibition is reported to be pleckstrin homology (PH) domain-dependent. It does not exhibit any inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50uM. Overcomes Akt1/Akt2-mediated resistance to chemotherapeutics in tumor cells and is shown to block basal and stimulated phosphorylation/activation of Akt1/Akt2 both in cultured cells in vitro and in mice in vivo.
Solubility:
DMSO (5mg/ml)
Molecular Weight:
~551.6
Storage and Stability:
May be stored at 4 degrees C. For long-term storage, aliquot and store at 4 degrees C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer. This product is light sensitive.