MK-2206 2HCl is a highly selective inhibitor of Akt1, Akt2, and Akt3 with IC50 values of 8 nM, 12 nM and 65 nM, respectively. MK-2206 is an allosteric inhibitor and is activated by the pleckstrin homology domain. MK-2206 inhibits auto-phosphorylation of b
Storage Temp
Store at -20°C,Argon charged
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
ALLOSTERIC MODULATOR
Mechanism of action
Allosteric modulator of AKT serine/threonine kinase 1;Allosteric modulator of AKT serine/threonine kinase 2;Allosteric modulator of AKT serine/threonine kinase 3
Product Description
MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively; no inhibitory activities against 250 other protein kinases observed. A highly selective pan-Akt inhibitor activated by the pleckstrin homology domain
1.Hirai H, Sootome H, Nakatsuru Y, Miyama K, Taguchi S, Tsujioka K, Ueno Y, Hatch H, Majumder PK, Pan BS et al.. (2010) MK-2206, an allosteric Akt inhibitor, enhances antitumor efficacy by standard chemotherapeutic agents or molecular targeted drugs in vitro and in vivo.. Mol Cancer Ther, 9 (7):(1956-67). [PMID:20571069][10.1021/op500134e]
2.Liu R, Liu D, Trink E, Bojdani E, Ning G, Xing M. (2011) The Akt-specific inhibitor MK2206 selectively inhibits thyroid cancer cells harboring mutations that can activate the PI3K/Akt pathway.. J Clin Endocrinol Metab, 96 (4):(E577-85). [PMID:21289267][10.1021/op500134e]
3.Lin YH, Chen BY, Lai WT, Wu SF, Guh JH, Cheng AL, Hsu LC. (2015) The Akt inhibitor MK-2206 enhances the cytotoxicity of paclitaxel (Taxol) and cisplatin in ovarian cancer cells.. Naunyn Schmiedebergs Arch Pharmacol, 388 (1):(19-31). [PMID:25164962][10.1021/op500134e]
4.Holland WS, Chinn DC, Lara Jr PN, Gandara DR, Mack PC. (2015) Effects of AKT inhibition on HGF-mediated erlotinib resistance in non-small cell lung cancer cell lines.. J Cancer Res Clin Oncol, 141 (4):(615-26). [PMID:25323938][10.1021/op500134e]
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H2203478