MK-2206 | 1888

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.

MK-2206 is 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).

1888 | MK-2206 DataSheet

Alternate Name/Synonyms: 8-(4-(1-Aminocyclobutyl)phenyl-9-phenyl[1,2,4]triazolo[3,4-f][1,6]naphthyridin-3(2H)-one dihydrochloride

Appearance: Crystalline solid

Formulation: N/A

CAS Number: 1032350-13-2

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₂₅H₂₁N₅O .2HCl

Molecular Weight: 480.39

Cell-Permeable?: Yes

Purity: ≥98% by HPLC

Solubilities: DMSO

Handling: Protect from air and moisture

Country of Origin: USA

Tag Line: An allosteric Akt inhibitor

MDL Number: MFCD12912151

PubChem CID: 46930998

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