产品描述

SC66 is an allosteric inhibitor which displays a dual-inhibitory function toward AKT activity with IC50 values of 0.77, 2.85 and 0.47 μg/ml in HepG2, Huh7 and Hep3B cells after 72 h treatment, respectively.

靶点（IC50 & Targe）

Akt

体外研究

SC66 reduces cell viability in a dose- and time-dependent manner, inhibits colony formation and induces apoptosis in HCC cells. SC66 treatment leads to a reduction in total and phospho-AKT levels. This is associated with alterations in cytoskeleton organization, a reduction in expression levels of E-cadherin, β-catenin and phospho-FAK, together with up-regulation of Snail protein levels. In addition, SC66 induces the production of reactive oxygen species (ROS) and DNA damage. SC66 affects AKT/mTOR signaling in HCC cell lines[1].

体内研究

In the mouse xenograft tumor model of Hep3B cells, SC66 treatment significantly reduces tumor volume to 37% on day 17 of treatment when compared with tumors in the untreated group. The inhibition of cell growth correlates with a reduction in phospho-AKT levels in the tumors of animals treated with SC66[1].

细胞实验

Cell lines: The human hepatocarcinoma cell lines HepG2, Huh7, PLC/PRF/5, Hep3B and HA22T/VGH cells

Concentrations: 2 and 4 μg/ml

Incubation Time: 1, 3 and 6 hours

Method: Caspase activity assays: Cells (2 × 104/well) are treated with 2 and 4 μg/ml SC66 and after 1, 3 and 6 hours the levels of caspase3/7 activities in the cells are measured by the Caspase-Glo® 3/7 Assay. Results are expressed as relative luminescence units (RLU). Values are the mean ± SD of two separate experiments, each performed in duplicate.

(Only for Reference)

动物实验

Animal Models: Male nude athymic mice (Fox1 nu/nu) aged 4 weeks inoculated with Hep3B cells at the right flank

Formulation: suspended in DMSO, further diluted in a solution of 25% ethanol

Dosages: 5 and 25 mg/kg

Administration: i.p.

(Only for Reference)

参考文献

[1] Cusimano A, et al. Oncotarget. 2015, 6(3):1707-22.