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  2. Stem Cell/Wnt PI3K/Akt/mTOR Autophagy Apoptosis
  3. Organoid Akt Autophagy Apoptosis
  4. MK-2206 dihydrochloride

MK-2206 dihydrochloride  (Synonyms: MK-2206 (2HCl))

目錄號: HY-10358 純度: 99.93%
COA 產(chǎn)品使用指南 技術(shù)支持

MK-2206 dihydrochloride (MK-2206 (2HCl)) 是一種具有口服活性的，可透過血腦屏障的，變構(gòu) Akt 抑制劑，對 Akt1、Akt2 和 Akt3 的 IC50 分別為 8、12 和 65 nM。許多乳腺癌細(xì)胞系、PIK3CA 突變體和 PTEN 丟失細(xì)胞系對 MK-2206 dihydrochloride 敏感。MK-2206 dihydrochloride 誘導(dǎo)自噬，具有抗癌活性。

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MK-2206 dihydrochloride Chemical Structure

MK-2206 dihydrochloride Chemical Structure

CAS No. : 1032350-13-2

1.  客戶無需承擔(dān)相應(yīng)的運輸費用。

2.  同一機構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機構(gòu)（單位）一年內(nèi)

     可免費申領(lǐng)三個不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥898
In-stock
1 mg ￥373
In-stock
5 mg ￥850
In-stock
10 mg ￥1172
In-stock
25 mg ￥2025
In-stock
50 mg ￥2900
In-stock
100 mg ￥4100
In-stock
200 mg 現(xiàn)貨 詢價
500 mg 現(xiàn)貨 詢價
1 g   詢價  
5 g   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of MK-2206 dihydrochloride:

MCE 顧客使用本產(chǎn)品發(fā)表的 353 篇科研文獻(xiàn)

WB
IF

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

    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.

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

    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: Cancer Cell. 2018 Jun 11;33(6):1061-1077.e6.  [Abstract]

    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: Nat Commun. 2018 May 8;9(1):1816.  [Abstract]

    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: Acta Pharmacol Sin. 2018 Nov;39(11):1787-1796.  [Abstract]

    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: Cell Death Dis. 2018 Oct 3;9(10):1015.  [Abstract]

    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: Clin Epigenetics. 2018 May 23;10:69.  [Abstract]

    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: Cancer Sci. 2018 Apr;109(4):944-955.  [Abstract]

    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: J Cell Biochem. 2018 May;119(5):3885-3891.  [Abstract]

    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: Int J Biochem Cell Biol. 2018 Jun;99:43-51.  [Abstract]

    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: Radiat Res. 2018 Aug;190(2):204-215.  [Abstract]

    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: J Cancer. 2018 Jun 14;9(14):2480-2491.  [Abstract]

    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: Br J Cancer. 2017 Sep 26;117(7):974-983.  [Abstract]

    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: Hum Mol Genet. 2017 Sep 15;26(18):3553-3563.  [Abstract]

    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: Oncotarget. 2017 Jan 31;8(5):8536-8549.  [Abstract]

    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.  [Abstract]

    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: 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: Proc Natl Acad Sci U S A. 2016 Jul 26;113(30):E4338-47.  [Abstract]

    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: 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: 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: Cell. 2014 Feb 13;156(4):771-85.  [Abstract]

    (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.

    查看 Akt 亞型特異性產(chǎn)品:

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active, BBB-penetrated allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy[1][2].

    IC50 & Target[1]

    Akt1

    8 nM (IC50)

    Akt2

    12 nM (IC50)

    Akt3

    65 nM (IC50)

    體外研究
    (In Vitro)

    MK-2206 dihydrochloride (0-10 μM；72 和 96 小時) 以劑量和時間依賴性方式抑制鼻咽癌 (NPC) 細(xì)胞系 CNE-1、CNE-2、HONE-1 和 SUNE-1 增值[1]。
    MK-2206 dihydrochloride (0-10 μM；24 和 48 小時) 導(dǎo)致 CNE-2 和 HONE-1 細(xì)胞中 G0/G1 期細(xì)胞百分比呈劑量依賴性增加，并伴隨 S 期細(xì)胞數(shù)量減少[2]。
    MK-2206 dihydrochloride (0-10 μM；24 小時) 以劑量依賴的方式減弱 PRAS40 和 S6 的磷酸化水平，不影響 GSKα/β 和 AKT 的磷酸化[2]。
    MK-2206 dihydrochloride (0-10 μM；24 小時) 劑量依賴性地增加 CNE-2 細(xì)胞中 LC3-II 的出現(xiàn)。微管相關(guān)蛋白 1 LC3 是一種必需的自噬蛋白[2]。

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

    Cell Proliferation Assay[2]

    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[2]

    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[2]

    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[2]

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

    MK-2206 dihydrochloride (MK-2206 (2HCl)) (口服灌胃；480 mg/kg 每周一次和 240 mg/kg 每周三次；持續(xù) 2 周) 均可抑制人 CNE-2 異種移植物的雄性 BALB/c 裸鼠。在小鼠中未觀察到其他明顯毒性[3]。
    MK-2206 dihydrochloride (口服灌胃；120 mg/kg；隔天；持續(xù) 3 周) 顯著抑制 3-5 周齡無胸腺裸鼠 GEO 結(jié)腸癌細(xì)胞的腫瘤生長[4]。

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

    Animal Model: Four- to 6-week-old male BALB/c nude mice with CNE-2 xenografts[2]
    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.
    Clinical Trial
    分子量

    480.39

    Formula

    C25H23Cl2N5O
    CAS 號
    性狀

    固體

    顏色

    Light yellow to green yellow

    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性數(shù)據(jù)
    細(xì)胞實驗： 

    DMSO 中的溶解度 : 12.5 mg/mL (26.02 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗：

    請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1.67 mg/mL (3.48 mM); 澄清溶液

      此方案可獲得 ≥ 1.67 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 16.7 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 1.67 mg/mL (3.48 mM); 澄清溶液

      此方案可獲得 ≥ 1.67 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 16.7 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。

    以下溶解方案，請直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

    • 方案 一

      請依序添加每種溶劑： 20% SBE-β-CD in Saline

      Solubility: 25 mg/mL (52.04 mM); 澄清溶液; 超聲助溶

    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.99%

    參考文獻(xiàn)

    MK-2206 dihydrochloride 相關(guān)分類

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0816 mL 10.4082 mL 20.8164 mL 52.0410 mL
    5 mM 0.4163 mL 2.0816 mL 4.1633 mL 10.4082 mL
    10 mM 0.2082 mL 1.0408 mL 2.0816 mL 5.2041 mL
    15 mM 0.1388 mL 0.6939 mL 1.3878 mL 3.4694 mL
    20 mM 0.1041 mL 0.5204 mL 1.0408 mL 2.6021 mL
    25 mM 0.0833 mL 0.4163 mL 0.8327 mL 2.0816 mL
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    產(chǎn)品名稱：
    MK-2206 dihydrochloride
    目錄號：
    HY-10358
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