MK-2206 2HCl - Moligand™, 10mM in DMSO , Allosteric modulator of AKT serine/threonine kinase 1;Allosteric modulator of AKT serine/threonine kinase 2;Allosteric modulator of AKT serine/threonine kinase 3, CAS No.1032350-13-2, Allosteric modulator of AKT serine/threonine kinase 1;Allosteric modulator of AKT serine/threonine kinase 2;Allosteric modulator of AKT serine/threonine kinase 3

CAS: 1032350-13-2 Cat. No.: M408752 Molecular Weight: 480.39 PubChem CID: 46930998

GRADE & PURITY Moligand™, 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

In vitro

MK-2206 is an allosteric inhibitor and is activated by the pleckstrin homology domain. MK-2206 inhibits auto-phosphorylation of both Akt T308 and S473. MK-2206 also prevents Akt-mediated phosphorylation of downstream signaling molecules, including TSC2, PRAS40 and ribosomal S6 proteins. MK-2206 inhibits Ras wild-type (WT) cell lines (A431, HCC827, and NCI-H292) more potently when compared to Ras-mutant cell lines (NCI-H358, NCI-H23, NCI-H1299, and Calu-6). MK-2206 also shows synergistic responses in combination with cytotoxic agents such as erlotinib or lapatinib in lung NCI-H460 or ovarian A2780 tumor cells. MK-2206 or siRNA-mediated Akt inhibition strongly activates autophagy in human glioma cells. However, eukaryotic elongation factor-2 (eEF-2) silencing suppresses MK-2206-induced-autophagy, with a promotion of apoptotic cell death.

In vivo

MK-2206 shows 60% TGI and inhibits more than 70 % of phospho-Akt1/2 (T308 and S473) in A2780 ovarian cancer xenografts at a dose of 240 mg/kg. MK-2206 exhibits significant antitumor activity in NCI-H292 xenograft in combination with erlotinib or lapatinib.
Cell Data

cell lines：tumor (HT1080, RCC45, MiaPaca) and normal cells (Wi38, NKE-hTERT)

Concentrations：0, 0.3, 1 and 3 μM

Incubation Time：72 or 96 hours

Powder Purity:≥99%

Specifications

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. MK-2206 2HCl induces autophagy and apoptosis in cancer cells. Ph

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

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

Names and Identifiers

• Isomeric SMILES: C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C4=NNC5=O)C6=CC=CC=C6)N.Cl.Cl
• PubChem CID: 46930998
• Molecular Weight: 480.39

Associated Targets(Human)

AKT3 Tchem RAC-gamma serine/threonine-protein kinase (1 Activities)

Discover Target: AKT3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AKT2 Tchem RAC-beta serine/threonine-protein kinase (1 Activities)

Discover Target: AKT2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AKT1 Tchem RAC-alpha serine/threonine-protein kinase (1 Activities)

Discover Target: AKT1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro Water: 3 mg/mL (10.74 mM); DMSO: Insoluble; Ethanol: Insoluble
• Melt Point(°C): >225°C

References

1. Huang Hongli, Chai Yihan, Wu Xuewei, Wang Sen, Li Binglin, Wang Yanyan, Zheng Wen, Wu Yuefeng, Meng Di, Wang Hua, Tu Zhengliang, Du Chengli, Lyu Xiayi, Li Guiying, Guo Wei.  (2025)  Non-canonical NOTCH1 signaling regulates ferroptosis vulnerability in dormant lung cancer cells with stable resistance.  Cell Death & Disease,      [PMID:41453945] [10.1038/s41419-025-08355-9]