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 Formula: C₂₅H₂₁N₅O·2HCl Peso molecolare: 480.39 PubChem CID: 46930998

GRADE & PURITY Moligand™, 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

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

Specifiche e purezza

Moligand™, 10mM in DMSO

Meccanismi biochimici e fisiologici

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

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Grado

Moligand™

Tipo di azione

ALLOSTERIC MODULATOR

Meccanismo d'azione

Allosteric modulator of AKT serine/threonine kinase 1;Allosteric modulator of AKT serine/threonine kinase 2;Allosteric modulator of AKT serine/threonine kinase 3

Nomi e identificatori

• Isomeri 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
• Peso molecolare: 480.39

Obiettivi associati (umani)

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)

Proprietà chimiche e fisiche

• Solubilità: Solubility (25°C) In vitro Water: 3 mg/mL (10.74 mM); DMSO: Insoluble; Ethanol: Insoluble
• Punto di fusione (°C): >225°C

Riferimenti

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]

2. Wenting Zhang, Minyan Qian, Wenwei Jiang, Jie Chen, Nan Hu, Jingting Jiang.  (2026)  Deciphering the Potential Mechanism of Cordycepin in Alleviating Ulcerative Colitis via the AKT1 Signaling Pathway: An Integrated Approach Combining Network Pharmacology, Molecular Docking, and Experimental Validation.  Journal of Inflammation Research,      [PMID:42609839] [10.2147/JIR.S599071]