10-DEBC hydrochloride,925681-4

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抑制剂描述：

产品名称：10-DEBC hydrochloride

产品别名：见爱必信官网

英文别名：10-DEBC hydrochloride

靶点：Others

CAS：925681-41-0

纯度：≥95%

外观：见爱必信官网

保存方法：Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

描述：

10-DEBC hydrochloride is a selective inhibitor of Akt (or termed PKB) , with an IC50 value of approximate 48 μM .

溶解性：Soluble in water (100 mM), and DMSO (100 mM).

体外研究：

As demonstrated by LDH and MTT tests, 10-DEBC dihydrochloride at 10 μM did not affect cell viability when it was applied alone. 10-DEBC dihydrochloride at this concentration in cisplatin-treated U251 cells abrogated the cytoprotective effect of metformin. 10-DEBC dihydrochloride showed neutralization effect on the antiapoptotic activity of metformin, increasing the cell membrane phosphatidylserine exposure and DNA fragmentation to the levels observed with cisplatin alone. In U251 cells, 10-DEBC dihydrochloride significantly induced the production of reactive oxygen species. In cisplatin-treated cells, 10-DEBC dihydrochloride consequently reduced the antioxidative effect of metformin.

体内研究：Studies in effects of 10-DEBC hydrochloride on BAT explants incubated with phentolamine were carried out. Without any effect on total Akt protein, 10-DEBC hydrochloride inhibited the phosphorylation of Akt Ser473 by ~40%. In WT explants, the 10-DEBC hydrochloride alone had no effect on the phosphorylation of Ser485/491 of AMPK, and did not affect the phentolamine effect. However, in β-AR KO explants, 10-DEBC hydrochloride blunted the AMPK Ser485/491 phosphorylation increased by phentolamine.

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