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))

目录号: HY-10358 纯度: 99.99%
COA 产品使用指南

摩尔计算器

MK-2206 dihydrochloride (MK-2206 (2HCl)) 是一种具有口服活性的，可透过血脑屏障的，变构 Akt 抑制剂，对 Akt1、Akt2 和 Akt3 的 IC50 分别为 8、12 和 65 nM。许多乳腺癌细胞系、PIK3CA 突变体和 PTEN 丢失细胞系对 MK-2206 dihydrochloride 敏感。MK-2206 dihydrochloride 诱导自噬，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

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥935
In-stock
5 mg ￥850
In-stock
10 mg ￥1172
In-stock
50 mg ￥2900
In-stock
100 mg ￥4100
In-stock
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500 mg   询价  

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Customer Review

Other Forms of MK-2206 dihydrochloride:

MK-2206 dihydrochloride 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 288 篇科研文献

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: 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: 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: 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: 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: 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: 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 亚型特异性产品:

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    Akt Akt1 Akt2 Akt3

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    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)

    体外研究
    (In Vitro)

    MK-2206 dihydrochloride (0-10 μM；72 和 96 小时) 以剂量和时间依赖性方式抑制鼻咽癌 (NPC) 细胞系 CNE-1、CNE-2、HONE-1 和 SUNE-1 增值[1]。
    MK-2206 dihydrochloride (0-10 μM；24 和 48 小时) 导致 CNE-2 和 HONE-1 细胞中 G0/G1 期细胞百分比呈剂量依赖性增加，并伴随 S 期细胞数量减少[2]。
    MK-2206 dihydrochloride (0-10 μM；24 小时) 以剂量依赖的方式减弱 PRAS40 和 S6 的磷酸化水平，不影响 GSKα/β 和 AKT 的磷酸化[2]。
    MK-2206 dihydrochloride (0-10 μM；24 小时) 剂量依赖性地增加 CNE-2 细胞中 LC3-II 的出现。微管相关蛋白 1 LC3 是一种必需的自噬蛋白[2]。

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

    MK-2206 dihydrochloride 相关抗体:

    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.
    体内研究
    (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；持续 2 周) 均可抑制人 CNE-2 异种移植物的雄性 BALB/c 裸鼠。在小鼠中未观察到其他明显毒性[3]。
    MK-2206 dihydrochloride (口服灌胃；120 mg/kg；隔天；持续 3 周) 显著抑制 3-5 周龄无胸腺裸鼠 GEO 结肠癌细胞的肿瘤生长[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 号
    性状

    固体

    颜色

    Light yellow to green yellow

    运输条件

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

    4°C, sealed storage, away from moisture

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

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 12.5 mg/mL (26.02 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    H2O 中的溶解度 : 3.57 mg/mL (7.43 mM; 超声助溶 (<60°C))

    配制储备液
    浓度 溶剂体积 质量 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
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

      此方案可获得 ≥ 1.67 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

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

      此方案可获得 ≥ 1.67 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

    以下溶解方案，请直接配置工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比； 如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂： 20% SBE-β-CD in Saline

      Solubility: 25 mg/mL (52.04 mM); 澄清溶液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。

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

    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.99%

    COA (197 KB) HNMR (279 KB) LCMS (89 KB)

    产品使用指南 (1538 KB)
    参考文献

    MK-2206 dihydrochloride 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    H2O / 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
    DMSO 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

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    MK-22061032350-13-2MK-2206 (2HCl)MK2206MK 2206OrganoidAktAutophagyApoptosisPKBProtein kinase BoralselectivebreastcancerPIK3CAmutantPTENlosssensitiveInhibitorinhibitorinhibit

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