AKT inhibitor VIII 是一种细胞渗透的喹喔啉化合物，可逆的选择性抑制Akt1、Akt2和Akt3的活性，IC50值分别为 58 nM、210 nM 和 2119 nM。

AKT inhibitor VIII is a highly specific Akt1/2 inhibitor (IC50: 58/210 nM). The selectivity for Akt1 is higher about 36-fold than Akt3.

Akti-1/2 (50 mg/kg,i.p.)抑制小鼠肺中基底和IGF-刺激的Akt1/2磷酸化作用.

在基于细胞的IPKA (C33A)试验中,AKT inhibitor VIII可抑制Akt1/2（IC50：305/2086 nM）。在MCF7,HT29和A2780细胞中,AKT inhibitor VIII可使caspase-3活性急剧增加从而诱导细胞凋亡。在肝细胞中,AKT inhibitor VIII可阻断胰岛素对PEPCK的调节,以及G6Pase表达和FOXO1活性。AKT inhibitor VIII通过阻断PKB还可使PAR-1-介导的血小板聚集显著增强。在HCC827,NCI-H522,NCI-1651和PC-9细胞中,AKT inhibitor VIII抑制细胞生长（IC50：4.7/7.25/9.5 μM）,AKT inhibitor VIII与gefitinib联用会增强对细胞生长和凋亡的抑制。

Kinase screen: Briefly, all assays (25.5 μl at 21°C for 30 min) are performed using a Biomek 2000 Laboratory Automation Workstation in a 96-well format. Reactions contains 5–20 mU purified kinase along with substrate peptide or protein and are initiated by the addition of 10 mM MgAcetate and 5, 20, or 50 μM ATP ([γ-33P]-ATP, 800 cpm/pmol).

The cell growth inhibitory effect of AKTi-1/2 is studied using the 96 h sulforhodamine B assay (SRB). Drug concentrations that inhibited 50% of cell growth (IC50) are calculated for each compound in GraphPad Prism 6.0 using non-linear regression analysis and sigmoidal dose–response (variable slope) equation.(Only for Reference)

612847-09-3

C34H29N7O

551.64

AKTi-1/2

DMSO:11 mg/mL (20 mM)),with gentle warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years