可以用于小胶质细胞的有:MK-2206;AT7867;CCT128930; 已经用于临床试验的有MK-2206 现给大家介绍一下主要的AKT抑制剂: MK-2206:a highly selective, potent non-ATP competitive allosteric Akt inhibitor with IC50 of 8 nM,12 nM, 65 mM for Akt1, Akt2 and Akt3 respectively; The phase II clinical trials of MK-2206 against the treatment of endometrial cancer are recruiting participant Dana-Farber Cancer Institute. Perifosine:A p.o.-bioavailable ALK(Alkylphospholipids),inhibits Akt activation。 AT7867 is a potent and oral AKT and p70 S6 kinase inhibitor with an IC50 of 17 nM. GSK690693:selective for the Akt isoforms(inhibits Akt kinases 1, 2, and 3 with IC50 values of 2, 13, and 9 nM respectively)。 PHT-427:inhibited Akt and PDPK1 signaling and their downstream targets. CCT128930:a novel potent ATP-competitive, AKT inhibitor with an IC50 of 6 nM. Palomid 529 (P529) a novel potent antitumour PI3K/Akt/mTOR inhibitor with a GI50 of <35 μM in the NCI-60 cell lines panel. Triciribine phosphate (NSC-280594):prevents the phosphorylation of Akt. A-674563: a potent selective protein kinase B/Akt inhibitor with an IC50 of 14 nM. A-674563 also shows inhibitory activity against PKA and CDK2 with IC50 of 16 and 46 nM, respectively. Triciribine: selectively inhibits the phosphorylation and activation of Akt1, -2 and -3.
|