Akt-I-1 [473382-39-7]

SYNkinase

Akt-I-1 [473382-39-7]

10

473382-39-7

Research Use Only

>95%

C22H30N6

378.5

Chemical. CAS: 473382-39-7. Formula: C22H30N6. MW: 378.5. The compound (Akt-I-1) inhibits only Akt1 (IC(50) 4.6 microM) 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. - The compound (Akt-I-1) inhibits only Akt1 (IC(50) 4.6 microM) 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.

2°C to 8°C

51202000