1. PI3K/Akt/mTOR
    Autophagy
    Apoptosis
  2. Akt
    Autophagy
    Apoptosis
  3. MK-2206

MK-2206 

Cat. No.: HY-108232
Handling Instructions

MK-2206 is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206. Anticancer activities.

For research use only. We do not sell to patients.

MK-2206 Chemical Structure

MK-2206 Chemical Structure

CAS No. : 1032349-77-1

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Top Publications Citing Use of Products

Publications Citing Use of MCE MK-2206

    MK-2206 purchased from MCE. Usage Cited in: Department of Dental Pharmacology. Okayama University. 2015.

    The role of Semaphorin4D in bone invasion by oral cancer.

    MK-2206 purchased from MCE. Usage Cited in: Br J Cancer. 2017 Sep 26;117(7):974-983.

    The effect of the AKT inhibitor MK2206 (10 μM) on the expression levels of phosphor-AKT, AKT, and STMN1 in TKI-pretreated NCI-H460 cells. β-actin is used as a loading control.

    MK-2206 purchased from MCE. Usage Cited in: Cell. 2014 Feb 13;156(4):771-85.

    (A) Effects of inhibiting PI3K and Akt in MEFs. Serum starved (16 hr) MEFs are pretreated (30 min) with Wortmannin (100 nM), MK2206 (2 μM) or vehicle (DMSO). Immunoblots of lysates are probed with the indicated antibodies. (B) PTEN null MEFs exhibit constitutive Akt, TSC2 and S6K phosphorylation, which are reversed by the Akt inhibitor MK2206.

    MK-2206 purchased from MCE. Usage Cited in: Proc Natl Acad Sci U S A. 2016 Jul 26;113(30):E4338-47.

    HCC1937 cells are treated for 16 h with inhibitors as indicated. Immunoblotting of total cell lysates is performed with antibodies as indicated. Induction of PAR and H2ax phosphorylation (γH2ax) following treatment with inhibitors of pan-PI3K (BKM120, 1.5 μM), PI3Kα (BYL719, 3 μM; PIK75, 0.5 μM), PI3Kβ (TGX221, 30 μM), AZD2281 (5 μM), and inhibitors of AKT (MK2206, 1 μM), SGK (GSK650394, 10 μM), or MAPKK (GSK1120212, 5 nM).

    MK-2206 purchased from MCE. Usage Cited in: Oncotarget. 2017 Jan 31;8(5):8536-8549.

    Western blot analysis of cyclin D1 and cyclin E in OE19 cells treated with the control, BIBR 277 alone, MK-2206 alone, or BIBR 277 combined with MK-2206 for 48 h.

    MK-2206 purchased from MCE. Usage Cited in: Oncotarget. 2017 Jul 18;8(29):47642-47654.

    Akt/JNK signal pathway is impaired in the inhibition of αMSH on adipocyte inflammation and FoxOs expressions. Mouse adipocytes are pretreated with αMSH and MK-2206, respectively. Relative protein levels of Akt, p-Aktser473, JNK, p-JNKThr183 with or without MK-2206 (n=3).

    MK-2206 purchased from MCE. Usage Cited in: Int J Biochem Cell Biol. 2018 Jun;99:43-51.

    Western blot analysis of NDRG2, p-ATK, XIAP, E-cadherin and Vimentin in TE-13 cells shows NDRG2 negatively regulates the expressions of AKT, XIAP, E-cadherin and Vimentin proteins.

    MK-2206 purchased from MCE. Usage Cited in: Cancer Sci. 2018 Apr;109(4):944-955.

    Western blotting of Sox2 and b-actin in A549 cells with or without IGF2 treated in the presence or absence of MK-2206.

    MK-2206 purchased from MCE. Usage Cited in: Nat Commun. 2018 May 8;9(1):1816.

    Representative western blot analysis of p-ERK1/2, p-p90 RSK, p-AKT, p-AKT p-PRAS40, p-FOXO1/3a/4, p-GSK3β, p-mTOR, p-p70 S6K, and p-S6 protein in MCF-10AP and MCF-10AH1047R cells stably expressing empty vector (EV) or mutant HRASQ61R treated with 2 µM MK2206 (AKTi) at different time points.

    MK-2206 purchased from MCE. Usage Cited in: Clin Epigenetics. 2018 May 23;10:69.

    The expression levels of E-cadherin, vimentin, pan-AKT, p-AKTser473, MMP-2, MMP-7, MMP-9, and actin (control) are detected by Western blot in RAI2 un-expressed and re-expressed RKO and LOVO cells as well as in the control group, shRAI2 knockdown group, and shRAI2 knockdown plus MK2206 treated group.

    MK-2206 purchased from MCE. Usage Cited in: Hum Mol Genet. 2017 Sep 15;26(18):3553-3563.

    Immunofluorescence analysis for expression of the I-cell marker ΔNP63 on proximal sections of ureters explanted from E12.5 wildtype (control) embryos and cultured for 6 d in the presence of solvent (DMSO) (A), the AKT inhibitor (AKT-i) MK2206 (B), the P38 inhibitor (P38-i) SB203580 (C), the ERK1/2 inhibitor (ERK1/2-i) PD98059 (D) or combinations as indicated (E and F).

    MK-2206 purchased from MCE. Usage Cited in: Cancer Cell. 2018 Jun 11;33(6):1061-1077.e6.

    Dih10 cells are treated with CDDP (20 μM) in the presence or absence of the Akt inhibitor MK2206 (5 μM).

    MK-2206 purchased from MCE. Usage Cited in: J Cancer. 2018 Jun 14;9(14):2480-2491.

    Analysis of indicated proteins in Cry1 silencing osteosarcoma cells after MK-2206 treatment. Data are expressed as the mean±standard deviation.

    MK-2206 purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2018 Nov;39(11):1787-1796.

    Effects of LY294002 or AKT siRNA on the levels of total AKT, pAKT, phosphorylated PRAS40 and pMDM2 are examined by Western blot analysis in MCF-7 cells when HBXIP was overexpressed. Effects of MK-2206 or HBXIP siRNA on the levels of total AKT, pAKT, pPRAS40, and pMDM2 are examined by Western blot analysis in MCF-7-HBXIP cells.

    MK-2206 purchased from MCE. Usage Cited in: J Invest Dermatol. 2019 Jan;139(1):71-80.

    HEKa (left) and HaCaT (right) cells are seeded in six-cell plates and pretreated with MK2206 for 6 hours, and then stimulated with M5 (2.5 ng/mL) for 48 hours before measuring the protein levels of cyclin D1, Akt, and phosphoAkt by Western blot analysis.

    MK-2206 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Oct 3;9(10):1015.

    Representative western blot images are showing the LC3, and the phosphorylated and total protein expression of Akt and ERK1/2 after treatment with H2O2 in the presence and absence of MK2206 (5 μM) and U0126 (25 μM).

    MK-2206 purchased from MCE. Usage Cited in: J Cell Biochem. 2018 May;119(5):3885-3891.

    Western blot showed the protein expression of P-gp,MRP1, PTEN, p-AKT, Bax, Bcl-2, and cleaved caspase-3.

    MK-2206 purchased from MCE. Usage Cited in: Radiat Res. 2018 Aug;190(2):204-215.

    When 6 Gy irradiation is combined with AKT2 inhibitor MK-2206 treatment, the protein levels in phosphorylated AKT2, mTOR and IKBa are decreased, and the downstream proapoptotic proteins, caspase 3 and caspase 8, are increased.

    MK-2206 purchased from MCE. Usage Cited in: Modern Oncology. 2017,25(01):0009-0013.

    The related protein expression of Bcl-2, Bax, Caspase-3, PARP, GSK-3β, p65 gene in each intervention group. Western blot assay:1:Control group; 2:MK2206 positive group; 3:0.3g/L Mat; 4: 0.6g/L Mat; 5:1.2g/LMat.

    MK-2206 purchased from MCE. Usage Cited in: Graduate School of Arts & Sciences. Harvard University. 2016 Aug.

    Mouse embryonic fibroblasts (MEFs) are deprived of Arginine and treated with 2 µM MK2206 for up to 6 hours.

    MK-2206 purchased from MCE. Usage Cited in: Oncogene. 2019 Jun;38(26):5250-5264.

    Western blotting analysis shows the effect of AKT inhibitor MK2206 (AKT i) and SET7 inhibitor (R)-PFI-2 on the levels of SOX2 proteins. The cells are treated with 1 μM MK2206 for 24 h and 10 μM (R)-PFI-2 for 12 h before being harvested for analysis.

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    Description

    MK-2206 is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206. Anticancer activities[1][2].

    IC50 & Target[1]

    Akt1

    8 nM ()

    Akt2

    12 nM ()

    Akt3

    65 nM ()

    In Vitro

    MK-2206 (0-10 μM; 72 and 96 hours) inhibits the nasopharyngeal carcinoma (NPC) cell lines CNE-1, CNE-2, HONE-1, and SUNE-1 proliferation in dose- and time-dependent manner[3].
    MK-2206 (0-10 μM; 24 and 48 hours) results in a dose-dependent increase in the percentage of cells in G0/G1 phase and a concomitant reduction of cell numbers in S phase in CNE-2 and HONE-1 cells[3].
    MK-2206 (0-10 μM; 24 hours) attenuates phosphorylation levels of PRAS40 and S6 in a dose-dependent manner. MK-2206 does not affect phosphorylation of GSKα/β and AKT[3].
    MK-2206 (0-10 μM; 24 hours) increases the appearance of LC3-II in CNE-2 cells dose-dependently. Microtubule-associated protein 1 LC3 is an essential autophagy protein[3].

    Cell Proliferation Assay[3]

    Cell Line: The NPC cell lines CNE-1, CNE-2, HONE-1, and SUNE-1
    Concentration: 0.08, 0.16, 0.31, 0.63, 1.25, 2.5, 5, 10 μM
    Incubation Time: 72 and 96 hours
    Result: At 72 and 96 hours, the IC50 values in CNE-1, CNE-2, and HONE-1 cell lines were 3-5 μM, and in SUNE-1, they were less than 1 μM.

    Cell Cycle Analysis[3]

    Cell Line: CNE-2 and HONE-1 cells
    Concentration: 0.625, 1.25, 2.5, 5, 10 μM
    Incubation Time: 24 or 48 hours
    Result: Induced cell cycle arrest at G1 in a dose-dependent manner.

    Western Blot Analysis[3]

    Cell Line: SUNE-1 and CNE-2 cells
    Concentration: 0.625, 1.25, 2.5, 5, 10 μM
    Incubation Time: 24 hours
    Result: Inhibited phosphorylation of AKT downstream targets.

    Cell Autophagy Assay[3]

    Cell Line: CNE-2 cells
    Concentration: 0.625, 1.25, 2.5, 5, 10 μM
    Incubation Time: 24 hours
    Result: Induced autophagy.
    In Vivo

    Both MK-2206 doses (oral gavage; 480 mg/kg once a week and 240 mg/kg three times a week; for 2 weeks) can inhibit the growth of human CNE-2 xenografts in nude mice. No other obvious toxicity is observed in mice[3].
    MK-2206 (orally; 120 mg/kg; alternate days; for 3 weeks) significantly inhibits tumor growth in 3-5 week old athymic nude mice with GEO colon carcinoma cells[4].

    Animal Model: Four- to 6-week-old male BALB/c nude mice with CNE-2 xenografts[3]
    Dosage: 240 mg/kg and 480 mg/kg
    Administration: Oral gavage; 240 mg/kg for three times a week; 480 mg/kg for once a week; for 2 weeks
    Result: Both doses inhibited the growth of human CNE-2 xenografts in nude mice.
    Molecular Weight

    443.93

    Formula

    C₂₅H₂₂ClN₅O

    CAS No.

    1032349-77-1

    SMILES

    O=C1NN=C2C3=C(N=C(C4=CC=C(C5(N)CCC5)C=C4)C(C6=CC=CC=C6)=C3)C=CN21.[H]Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
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    Keywords:

    MK-2206MK2206MK 2206AktAutophagyApoptosisPKBProtein kinase BoralselectivebreastcancerPIK3CAmutantPTENlosssensitiveInhibitorinhibitorinhibit

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