2. Neuronal Signaling Autophagy
  3. CaMK Autophagy
  4. KN-93

KN-93是可渗透细胞，可逆和竞争性的抑制剂钙调蛋白依赖性激酶II型 (CaMKII) 抑制剂，Ki 为370 nM。

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KN-93 Chemical Structure

KN-93 Chemical Structure

CAS No. : 139298-40-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1213
In-stock
1 mg ￥494
In-stock
5 mg   询价  
10 mg   询价  

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Customer Review

Other Forms of KN-93:

KN-93 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 63 篇科研文献

WB

    KN-93 purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2020 Feb;41(2):218-228.   [Abstract]

    HUVECs are pretreated with KN93 for 1 h, followed by ZYZ-803 (1 μM) for 30 min. Protein levels are assessed by Western blot.

    KN-93 purchased from MCE. Usage Cited in: Diabetes. 2018 Sep;67(9):1748-1760.  [Abstract]

    Immunoblotting analysis of PCK1, G6Pase, and phospho-CaMKIIγ proteins in NTG and HCTG hepatocytes in response to PGF2α and in the presence or absence of KN-93 treatment.

    KN-93 purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Apr 12;9:362.  [Abstract]

    MK 733-increased biotinylated α7nAChR protein is blocked by the addition of KN93 (P<0.01, n=6 mice).

    KN-93 purchased from MCE. Usage Cited in: Exp Cell Res. 2018 Mar 15;364(2):198-207.  [Abstract]

    Western blot analysis of β-catenin protein level in HEK 293T cells stimulated for 12h with rAGR2 (100 ng/mL) coupled with or without KN93 (10 μM).

    查看 CaMK 亚型特异性产品:

    查看所有亚型
    CaMK III CaMK II

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    KN-93 is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM.

    IC50 & Target

    CaMK II

     

    体外研究
    (In Vitro)

    After 2 days of KN-93 treatment, 95% of cells are arrested in G1. G1 arrest is reversible; 1 day after KN-93 release, a peak of cells had progressed into S and G2-M. KN-93 also blocks cell growth stimulated by basic fibroblast growth factor, platelet-derived growth factor-BB, and epidermal growth factor in NIH 3T3 fibroblasts[1]. KN-93 inhibits the H+, K+-ATPase activity but strongly dissipates the proton gradient formed in the gastric membrane vesicles and reduces the volume of luminal space[2]. KN-93 (0.5 μM) prevents increased LV developed pressure during action potential prolongation and early afterdepolarizations. Ca2+-independent CaM kinase activity is increased during early afterdepolarizations and this increase is prevented by KN-93[3]. KN-93 (10 μM )significantly inhibits the activation of CaMKII/NF-κB signaling induced by elevated glucose, and subsequently decreases the expression of VEGF, iNOS and ICAM-1 in Müller cells[4].

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

    KN-93 相关抗体:
    体内研究
    (In Vivo)

    KN-93 (1 mg/kg/day, i.p.) inhibits retinal vascular leakage induced by diabetes, and suppresses phosphorylation of CaMKII and NF-κB in diabetic retina[4].

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

    501.04

    Formula

    C26H29ClN2O4S
    CAS 号
    性状

    固体

    颜色

    White to off-white

    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 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 50 mg/mL (99.79 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)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.9958 mL 9.9792 mL 19.9585 mL
    5 mM 0.3992 mL 1.9958 mL 3.9917 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 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

    动物实验：

    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    90% Corn Oil

      Solubility: ≥ 0.83 mg/mL (1.66 mM); 澄清溶液

      此方案可获得 ≥ 0.83 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。

      以 1 mL 工作液为例，取 100 μL 8.3 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

    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）。
    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: 99.42%

    COA (292 KB) HNMR (262 KB) RP-HPLC (248 KB) LCMS (93 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [4]

    Cell viability is assessed by the 3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide (MTT) assay. Briefly, Müller cells are seeded at a density of 10×104 cells per well in 96-well plates and cultured until sub-confluence. Next, cells are treated with curcumin for 24 h before incubation with MTT (5 mg/mL) at 37°C in 5% CO2 atmosphere for 4 h. The culture medium is then removed, and the formazan formed in the reaction is dissolved in 150 μL DMSO. The optical density of the solution is measured at 490 nm using a multifunctional microplate reader. Cell viability in each well is presented as a percentage of the control (vehicle-treated group).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [4]

    Male Sprague-Dawley rats (8 weeks of age) weighing 180-200 g are used in this study. Rats are housed in ventilated microisolator cages with free access to water and food. The rats are randomLy assigned to receive either 60 mg/kg STZ intraperitoneally or citrate buffer alone. Rats are categorized as diabetic when blood glucose levels exceeded 16.7 mM at 48 h after STZ treatment. Two weeks after the induction of diabetes, rats are divided randomLy into three subgroups: STZ-diabetic rats (n=12), STZ-treated diabetic rats administered curcumin (n=12), or STZ-diabetic rats administered KN93 (n=12) for a 12-week period. Curcumin is suspended in saline containing 0.5% carboxymethylcellulose at a concentration of 20 mg/mL and administered via oral gavage at a total dose of 100 mg/kg/day. KN93 is administered by intraperitoneal injection at 1 mg/kg/day. Control STZ-treated diabetic rats and non-diabetic controls (n=12) are gavage administered saline containing 0.5% carboxymethylcellulose on a daily basis. Body weights and blood glucose levels are measured every 2 weeks.

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

    KN-93 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9958 mL 9.9792 mL 19.9585 mL 49.8962 mL
    5 mM 0.3992 mL 1.9958 mL 3.9917 mL 9.9792 mL
    10 mM 0.1996 mL 0.9979 mL 1.9958 mL 4.9896 mL
    15 mM 0.1331 mL 0.6653 mL 1.3306 mL 3.3264 mL
    20 mM 0.0998 mL 0.4990 mL 0.9979 mL 2.4948 mL
    25 mM 0.0798 mL 0.3992 mL 0.7983 mL 1.9958 mL
    30 mM 0.0665 mL 0.3326 mL 0.6653 mL 1.6632 mL
    40 mM 0.0499 mL 0.2495 mL 0.4990 mL 1.2474 mL
    50 mM 0.0399 mL 0.1996 mL 0.3992 mL 0.9979 mL
    60 mM 0.0333 mL 0.1663 mL 0.3326 mL 0.8316 mL
    80 mM 0.0249 mL 0.1247 mL 0.2495 mL 0.6237 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.

    Keywords:

    KN-93139298-40-1KN93KN 93CaMKAutophagyCalmodulin-dependent protein kinasesCalmodulin-dependent kinasesInhibitorinhibitorinhibit

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