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Chemdea |
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Akt Inhibitor VIII, Isozyme-Selective,
Akti-1/2 |
Catalog # CD0223 |
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Price: 1 mg - $95;
5 mg - $125; 10 mg - $195; 25 mg - $450 |
Availability: In stock |
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1,3-Dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one
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 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.
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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SAME PRODUCT AS: |
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Cat. No. 124018 |
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Cat. No.
A6730 (TFA salt) |
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CHEMDEA; |