1. PI3K/Akt/mTOR
    Autophagy
  2. Akt
    Autophagy
  3. MK 2206 dihydrochloride

MK 2206 dihydrochloride 

Cat. No.: HY-10358 Purity: 99.47%
Handling Instructions

MK 2206 dihydrochloride is an orally active allosteric Akt inhibitor with IC50s of 5, 12 and 65 nM for Akt1, Akt2 and Akt3, respectively.

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

MK 2206 dihydrochloride Chemical Structure

MK 2206 dihydrochloride Chemical Structure

CAS No. : 1032350-13-2

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 80 In-stock
Estimated Time of Arrival: December 31
50 mg USD 180 In-stock
Estimated Time of Arrival: December 31
100 mg USD 280 In-stock
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200 mg USD 450 In-stock
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Customer Review

Top Publications Citing Use of Products

Customer Validation

    MK 2206 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride purchased from MCE. Usage Cited in: Oncogene. 2019 Mar 20. 

    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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    • Biological Activity

    • Protocol

    • Technical Information

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    • References

    Description

    MK 2206 dihydrochloride is an orally active allosteric Akt inhibitor with IC50s of 5, 12 and 65 nM for Akt1, Akt2 and Akt3, respectively.

    IC50 & Target[1]

    Akt1

    5 nM (IC50)

    Akt2

    12 nM (IC50)

    Akt3

    65 nM (IC50)

    Autophagy

     

    In Vitro

    The NPC cell lines CNE-1, CNE-2, HONE-1, and SUNE-1 are treated with increasing doses of MK-2206 (0-10 μM) for 72 and 96 hours, results in dose- and time-dependent inhibition of cell viability. At 72 and 96 hours, the IC50 values of MK-2206 in CNE-1, CNE-2, and HONE-1 cell lines are 3-5 μM, and in SUNE-1, they are less than 1 μM[1]. MK-2206 alone more potently inhibits the cell growth of Ras wild-type (WT) cell lines (A431, HCC827, and NCI-H292; IC50s of 5.5, 4.3, and 5.2 μM, respectively) as compared with Ras-mutant cell lines (NCI-H358, NCI-H23, NCI-H1299, and Calu-6; IC50s of 13.5, 14.1, 27.0, and 28.6 μM, respectively), with the exception of NCI-H460, which has a PIK3CA E545K mutation (IC50, 3.4 μM)[2].

    In Vivo

    MK-2206 doses (480 mg/kg once a week and 240 mg/kg three times a week) can inhibit the growth of human CNE-2 xenografts in nude mice. In the two MK-2206 groups, the tumor weights are much lighter than the control group (P<0.01). Temporal body weight reduction is observed after receiving the MK-2206 treatment[1].

    Clinical Trial
    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 20 mg/mL (41.63 mM; Need ultrasonic)

    H2O : 3.81 mg/mL (7.93 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0816 mL 10.4082 mL 20.8164 mL
    5 mM 0.4163 mL 2.0816 mL 4.1633 mL
    10 mM 0.2082 mL 1.0408 mL 2.0816 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2 mg/mL (4.16 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2 mg/mL (4.16 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [1]

    The NPC cell lines CNE-1, CNE-2, HONE-1, and SUNE-1 are seeded into 96-well plates at an appropriate density per well. Twenty-four hours after plating, varying concentrations of MK-2206 (0-10 μM) are added to the wells. Cell proliferation is determined by using the Cell Counting Kit 8 at 72 or 96 hours after dosing. The optical density is measured at 450 nm on an enzyme-linked immunosorbent assay reader. The IC50 value is determined as the concentration resulting in 50% cell growth inhibition after a 72 or 96 hours exposure to the drug compared with untreated control cells. All experiments are performed in triplicate in at least three independent experiments[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Mice[1]
    Four- to six-week-old male BALB/c nude mice are used. CNE-2 cells at 1×107/mL are suspended in serum-free medium, and 0.2 mL medium is injected subcutaneously into the right flank of each nude mouse. When mean tumor volume reaches approximately 50 mm3, the mice are randomized into three groups (n=7/group) with approximately equivalent ranges of tumor volume between groups. The MK-2206 is dosed with 30% Captisol. MK-2206 (240 mg/kg, three times a week), MK-2206 (480 mg/kg, once a week), and 30% Captisol diluents are administered by oral gavage for 2 weeks for each group. Tumor growth is measured with calipers every other day, and the tumor volume is calculated by the following formula: volume (mm3)=length×width2×0.5. Mice are killed when mean tumor volume in the control group is larger than 2,000 mm3. Harvested tumor specimens are weighed and fixed in 10% buffered formalin and embedded in paraffin.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    480.39

    Formula

    C₂₅H₂₃Cl₂N₅O

    CAS No.

    1032350-13-2

    SMILES

    O=C1N2C(C3=CC(C4=CC=CC=C4)=C(N=C3C=C2)C5=CC=C(C6(N)CCC6)C=C5)=NN1.Cl.Cl

    Shipping

    Room temperature in continental US; may vary elsewhere

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    Product Name:
    MK 2206 dihydrochloride
    Cat. No.:
    HY-10358
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    MK 2206 dihydrochloride

    Cat. No.: HY-10358