AKT inhibitor VIII

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种选择性变构 Akt 抑制剂，对 Akt1/2 的 IC50 分别为 58/210。

A selective, allosteric Akt inhibitor with IC50 of 58/210 for Akt1/2 respectively; shows weak activity for Akt3 (IC50=2.12 uM); inhibits basal and IGF stimulated Akt1 and Akt2 phosphorylation in mouse lung, with no effect on Akt3 phosphorylation.

When LnCaP cells are pretreated with AKT inhibitor VIII and then incubated with TRAIL, a dramatic increase in caspase-3 activity (6-10-fold relative to control or TRAIL alone) is observed. This sensitization of tumor cell lines with AKT inhibitor VIII is not limited to LnCaP cells as similar apoptosis induction is observed in HT29, MCF7, and A2780 cells, among others, with chemosensitizers such as camptothecin, herceptin, and doxorubicin. The furanodiene-induced decrease of p-Akt and Akt expressions is enhanced by the Akt inhibitor VIII pretreatment. Furthermore, the furanodiene-induced PARP cleavage is enhanced by Akt inhibitor VIII pretreatment. The Akt inhibitor VIII shows no effect on cleaved PARP expression but decreases the p-Akt and Akt expressions. AKT inhibitor VIII decreases cell viability and increases phosphatidylserine (PS) translocation to the outer leaflet of the plasma membrane, DNA fragmentation, Caspase-9 cleavage, Caspase-3 activation and PARP proteolysis in hESC lines WA01 (H1) and WA09 (H9) and in a hiPSCs cell line generated in our laboratory (FN2.1).

Mice are dosed with AKT inhibitor VIII (50 mpk, 3 doses, ip, every 90 min) achieving plasma concentrations of 1.5-2.0 μM, and then the animals are tail vein injected with IGF to stimulate Akt phosphorylation. By IP Western, both basal and IGF stimulated Akt1 and Akt2 phosphorylation are inhibited in mouse lung, with no effect on Akt3 phosphorylation.

AKT inhibitor VIII | AKT-inhibitor-VIII | AKT inhibitor-8 | AKT-inhibitor-8 | Akt-I 1,2 | Akti-1/2. Sigma-A6730

Cytoskeleton/Cell Adhesion Molecules

Akt

Akt1|Akt2|Akt3

Cancer

——

612847-09-3

551.6404

C34H29N7O

>98% (HPLC)

10 mM in DMSO

O=C1N(C2CCN(CC3=CC=C(C4=NC5=CC6=C(N=CN6)C=C5N=C4C7=CC=CC=C7)C=C3)CC2)C8=CC=CC=C8N1

2H-Benzimidazol-2-one, 1,3-dihydro-1-[1-[[4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl]methyl]-4-piperidinyl]-

(-20℃)

With Ice Pack

≥ 2 years