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MK-2206

based on 1 citations in multiple journalsMK-220614.1 4
An allosteric Akt inhibitor
Catalog #: 1888
SKU-Size Size Price Qty
1888-500 500 µg
$98.00
1888-1000 1 mg
$175.00
More Sizes Get Quote

Product Details

Alternate Name 8-(4-(1-Aminocyclobutyl)phenyl-9-phenyl[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3(2H)-one dihydrochloride
Appearance Crystalline solid
CAS # 1032350-13-2
Molecular Formula C₂₅H₂₁N₅O .2HCl
Molecular Weight 480.39
Purity ≥98% by HPLC
Solubility DMSO
SMILES C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C4=NNC5=O)C6=CC=CC=C6)N.Cl.Cl
InChi InChI=1S/C25H21N5O.2ClH/c26-25(12-4-13-25)18-9-7-17(8-10-18)22-19(16-5-2-1-3-6-16)15-20-21(27-22)11-14-30-23(20)28-29-24(30)31;;/h1-3,5-11,14-15H,4,12-13,26H2,(H,29,31);2*1H
InChi Key HWUHTJIKQZZBRA-UHFFFAOYSA-N
PubChem CID 46930998
MDL Number MFCD12912151
Handling Protect from air and moisture
Storage Conditions -20°C
Shipping Conditions Gel Pack
USAGE For Research Use Only! Not For Use in Humans.

Details

A highly selective non-ATP competitive allosteric Akt inhibitor with IC₅₀’s of 8 nM, 2 nM and 65 nM for Akt1, Akt2 and Akt3, respectively. MK-2206 potently inhibits phosphorylation of Thr³⁰⁸ and Ser⁴⁷³ in 3T3-L1 adipocytes with IC₅₀ values of 0.11 and 0.18 µM, respectively as well as downstream effects of insulin on GLUT4 translocation (IC₅₀ = 0.47 µM) and glucose transport (IC₅₀ = 0.14 µM). In addition, treatment with MK-2206 causes a robust, concentration-dependent activation of autophagy in human glioma cell lines LN229 and T98G.


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Guan, Jian et al. (2016) Overexpression of caveolin-1 reduces Taxol resistance in human osteosarcoma cells by attenuating PI3K-Akt-JNK dependent autophagy, Exp Ther Med. 2016 Nov;12(5):2815-2822.
Cheng et al., The TWEAK Receptor Fn14 Is an Src-Inducible Protein and a Positive Regulator of Src-Driven Cell Invasion. Mol. Cancer Res., Mar 2015; 13: 575 - 583.
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