Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2-CAS 612847-09-3-Calbiochem

C₃₄H₂₉N₇O

551.64

A cell-permeable and reversible quinoxaline compound that potently and selectively inhibits Akt1/Akt2 activity (IC₅₀ = 58 nM, 210 nM, and 2.12 µM for Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays). The inhibition appears 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 50 µM. 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. A 10 mM (1 mg/181 µl) solution of Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 (Cat. No. 124017) in DMSO is also available.
A cell-permeable, reversible, potent, and selective inhibitor of Akt1/Akt2 activity (IC₅₀ = 58 nM, 210 nM, and 2.12 µM 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 50 µM. 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.

Primary Target
Akt1, Akt2, Akt3
Product does not compete with ATP.
Reversible: yes
Target IC₅₀: 58 nM, 210 nM, 2.12 µM against Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays
Cell permeable: yes

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.

Calleja, V., et al. 2009. PLoS Biol.7, e17.
Logie, L., et al. 2007. Diabetes56, 228.
Barnett, S.F., et al. 2005. Biochem. J.385, 399.
DeFeo-Jones, D., et al. 2005. Mol. Cancer Ther.4, 271.
Zhao, Z., et al. 2005. Bioorg. Med. Chem. Lett.15, 905.
Lindsley, C.W., et al. 2005. Bioorg. Med. Chem. Lett.15, 761.

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

200

≥95% (HPLC)

solid

Calbiochem^®

OK to freeze
protect from light

yellow

DMSO: 5 mg/mL

ambient

2-8℃

5 mg in Glass bottle
1 mg in Plastic ampoule
Packaged under inert gas

11 - Combustible Solids

WGK 3