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Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2

Catalog # CD0223

Price:  1 mg - $95; 5 mg - $125; 10 mg - $195; 25 mg - $450

Availability:  In stock





Light yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. Purity: 98% by HPLC. CAS # 612847-09-3. Solubility: DMSO (5 mg/mL). Molecular Formula: C34H29N7O. Molecular Weight: 551.6.



A cell-permeable quinoxaline compound that potently and selectively inhibits Akt1/Akt2 activity (IC50 = 58 nM, 210 nM, and 2.12 M 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 M. 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.


Reference: 1. Calleja, V., et al. PLoS Biol. 2009, 7, 189; 2. Logie, L., et al. Diabetes 2007, 56, 2218; 3. Barnett, S.F., et al. Biochem. J. 2005, 385, 399; 4. DeFeo-Jones, D., et al. Mol. Cancer Ther. 2005, 4, 271; 5. Zhao, Z., et al. Bioorg. Med. Chem. Lett. 2005, 15, 905; 6. Lindsley, C.W., et al. Bioorg. Med. Chem. Lett. 2005, 15, 761.





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Caution Not fully tested. For research use only. Not for human use.

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