Akt-I-2 hydrochloride [473382-48-8]

SYNkinase

Akt-I-2 hydrochloride [473382-48-8, 473382-50-2]

10

473382-48-8

Research Use Only

>95%

C23H21N3 . HCl

339.4 . 36.5

Chemical. CAS: 473382-50-2. Formula: C23H21N3 . HCl. MW: 339.4 . 36.5. The compound (Akt-I-2) inhibited both Akt1 and Akt2 with IC(50) values of 2.7 and 21 microM respectively. It does not inhibit 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 and AKT2 isoforms, AKT-I-1,2 blocked the phosphorylation and activation of AKT1 and AKT2 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-2) inhibited both Akt1 and Akt2 with IC(50) values of 2.7 and 21 microM respectively. It does not inhibit 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 and AKT2 isoforms, AKT-I-1,2 blocked the phosphorylation and activation of AKT1 and AKT2 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

12352200