124018
Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2
Akti-1/2, 1,3-Dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one
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EMD Chemicals, Inc.
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13 February 2012
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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.
| Product information | |||
|---|---|---|---|
| Form | Yellow solid | ||
| Primary Target | Akt1, Akt2, Akt3 | ||
| Primary Target IC50 | 58 nM, 210 nM, 2.12 µM respectively | ||
| Secondary target | PKA, PKC, SGK (all with IC50 = 50 µM) | ||
| Molar mass | 551.6 | ||
| Protect from Light | Yes | ||
| Packaged under inert gas | Yes | ||
| Cell permeable | Yes | ||
| Purity | ≥95% by HPLC | ||
| Solubility | DMSO | ||
| Chemical formula | C34H29N7O | ||
| CAS number | 612847-09-3 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | +2°C to +8°C | ||
| Ship |
Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Standard Handling |
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