1. PI3K/Akt/mTOR Apoptosis
  2. Akt Apoptosis
  3. AKT inhibitor VIII

AKT inhibitor VIII  (Synonyms: AKTi-1/2)

目录号: HY-10355 纯度: 98.74%
COA 产品使用指南

AKT inhibitor VIII (AKTi-1/2) 是一种细胞渗透的喹喔啉化合物,能够有效的,选择性的,可逆的抑制 Akt1Akt2Akt3 的活性,IC50 值分别为 58 nM,210 nM 和 2119 nM。

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AKT inhibitor VIII Chemical Structure

AKT inhibitor VIII Chemical Structure

CAS No. : 612847-09-3

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10 mM * 1 mL in DMSO ¥1456
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1 mg ¥545
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5 mg ¥1200
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10 mg ¥2000
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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 37 篇科研文献

WB

    AKT inhibitor VIII purchased from MCE. Usage Cited in: Nutrients. 2018 Sep 23;10(10). pii: E1366.  [Abstract]

    Competition tests of SC79, PHT-427, AT7867, and AKT inhibitor VIII with the CGA probe against enriched AKT by CGA-modified functionalized MMs. Bands of AKT are detected by Western blot.

    AKT inhibitor VIII purchased from MCE. Usage Cited in: Cell Death Dis. 2017 May 25;8(5):e2817.  [Abstract]

    Injury-induced follicular activation is blocked by the mTOR inhibitor rapamycin. Mice are treated with specific inhibitors of the signaling pathways 12 h before surgery and another injection is given just after the surgery. Ovaries are collected at 6 h or 3 weeks after the surgery. C, control ovaries; S, surgically treated ovaries; Rapamycin, mTORC1 inhibitor; Akt VIII, Akt inhibitor; U0126, MAPK inhibitor. Specific inhibition of corresponding signaling pathways by inhibitors. Ovaries are collec

    查看 Akt 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    AKT inhibitor VIII (AKTi-1/2) is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity with IC50s of 58 nM, 210 nM, and 2119 nM, respectively.

    IC50 & Target[1]

    Akt1

    58 nM (IC50)

    Akt2

    210 nM (IC50)

    Akt3

    2119 nM (IC50)

    体外研究
    (In Vitro)

    When LnCaP cells are pretreated with AKT inhibitor VIII and then incubated with TRAIL, a dramatic increase in caspase-3 activity (6-10-fold relative to control or TRAIL alone) is observed. This sensitization of tumor cell lines with AKT inhibitor VIII is not limited to LnCaP cells as similar apoptosis induction is observed in HT29, MCF7, and A2780 cells, among others, with chemosensitizers such as camptothecin, herceptin, and doxorubicin[1]. The furanodiene-induced decrease of p-Akt and Akt expressions is enhanced by the Akt inhibitor VIII pretreatment. Furthermore, the furanodiene-induced PARP cleavage is enhanced by Akt inhibitor VIII pretreatment. The Akt inhibitor VIII shows no effect on cleaved PARP expression but decreases the p-Akt and Akt expressions[2]. AKT inhibitor VIII decreases cell viability and increases phosphatidylserine (PS) translocation to the outer leaflet of the plasma membrane, DNA fragmentation, Caspase-9 cleavage, Caspase-3 activation and PARP proteolysis in hESC lines WA01 (H1) and WA09 (H9) and in a hiPSCs cell line generated in our laboratory (FN2.1)[3].

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

    体内研究
    (In Vivo)

    Mice are dosed with AKT inhibitor VIII (50 mpk, 3 doses, ip, every 90 min) achieving plasma concentrations of 1.5-2.0 μM, and then the animals are tail vein injected with IGF to stimulate Akt phosphorylation. By IP Western, both basal and IGF stimulated Akt1 and Akt2 phosphorylation are inhibited in mouse lung, with no effect on Akt3 phosphorylation[1].

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

    分子量

    551.64

    Formula

    C34H29N7O

    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 20 mg/mL (36.26 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.8128 mL 9.0639 mL 18.1278 mL
    5 mM 0.3626 mL 1.8128 mL 3.6256 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, 1 years; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    • 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: ≥ 2 mg/mL (3.63 mM); 澄清溶液

      此方案可获得 ≥ 2 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.0 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% Corn Oil

      Solubility: ≥ 2 mg/mL (3.63 mM); 澄清溶液

      此方案可获得 ≥ 2 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      1 mL 工作液为例,取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    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

    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)。
    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: 98.97%

    参考文献
    Cell Assay
    [3]

    PSC are plated onto Matrigel coated 96-well plates at densities between 1×103-3×105 cells per well and grown until confluence. 24 hours post-treatments, 50 μg/well of activated 2,3-bis (2-methoxy-4-nitro-5-sulfophenyl)-5 [(phenylamino) carbonyl]-2 H-tetrazolium hydroxide(XTT) in PBS containing 0.3 μg/well of N-methyl dibenzopyrazine methyl sulfate (PMS) are added (final volume 100 μL) and incubated for 1-2 hours at 37°C. Cellular metabolic activity is determined spectrophotometrically at 450 nm.

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

    参考文献

    AKT inhibitor VIII 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, 1 years; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6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
    DMSO 1 mM 1.8128 mL 9.0639 mL 18.1278 mL 45.3194 mL
    5 mM 0.3626 mL 1.8128 mL 3.6256 mL 9.0639 mL
    10 mM 0.1813 mL 0.9064 mL 1.8128 mL 4.5319 mL
    15 mM 0.1209 mL 0.6043 mL 1.2085 mL 3.0213 mL
    20 mM 0.0906 mL 0.4532 mL 0.9064 mL 2.2660 mL
    25 mM 0.0725 mL 0.3626 mL 0.7251 mL 1.8128 mL
    30 mM 0.0604 mL 0.3021 mL 0.6043 mL 1.5106 mL
    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.

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    产品名称:
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    目录号:
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