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AktI1

Chemical

C22H30N6

378.5

473382-39-7

≥95%

Solid.

Soluble in DMSO.

Manufactured by SynKinase.

Target: AKT | Kinase Group: AGC | Substrate: Serine-ThreonineClick here for Original Manufacturer Product DatasheetOur product description may differ slightly from the original manufacturers product datasheet.

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AMBIENT

+4°C

-20°C

Stable for at least 2 years after receipt when stored at -20°C.

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The compound (Akt-I-1) inhibits only Akt1 (IC(50) 4.6 µM) and does not inhibit AKT2, or AKT3. The compound is a reversible inhibitor, and exhibits a linear mixed-type inhibition against ATP and peptide substrate. In addition to inhibiting kinase activity of AKT1 isoform, AKT-I-1 blocked the phosphorylation and activation of AKT1 by PDK1 (phosphoinositide-dependent kinase 1). The inhibitor was found to be cell-active and to block phosphorylation of Akt at Thr308 and Ser473, reduce the levels of active Akt in cells, block the phosphorylation of known Akt substrates and promote TRAIL (tumour-necrosis-factor-related apoptosis-inducing ligand)-induced apoptosis in LNCap prostate cancer cells.Product References

Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors: S.F. Barnett, et al.; Biochem. J. 385, 399 (2005)

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