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

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

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CAS 番号 : 139298-40-1

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 160 在庫あり
Solution
10 mM * 1 mL in DMSO USD 160 在庫あり
Solid
1 mg $73 在庫あり
5 mg $145 在庫あり
10 mg $198 在庫あり
25 mg $390 在庫あり
50 mg $480 在庫あり
100 mg $700 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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カスタマーレビュー

Based on 95 publication(s) in Google Scholar

Other Forms of KN-93:

Top Publications Citing Use of Products

顧客検証

WB

    KN-93 purchased from MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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).

    CaMK アイソフォーム固有の製品をすべて表示:

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    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

     

    Cellular Effect
    Cell Line Type Value Description References
    Sf9 IC50
    1.6 3
    Compound: 1, KN-93
    Inhibition of recombinant CAMK2 expressed in Sf9 cells after 20 mins
    Inhibition of recombinant CAMK2 expressed in Sf9 cells after 20 mins
    [PMID: 21292482]
    Sf9 IC50
    1.6 3
    Compound: 1, KN-93
    Inhibition of recombinant CAMK2 expressed in Sf9 cells after 20 mins
    Inhibition of recombinant CAMK2 expressed in Sf9 cells after 20 mins
    [PMID: 21292482]
    NIH3T3 IC50
    12 3
    Compound: Chemical probe: KN-93
    Cytotoxicity against serum stimulated mouse NIH3T3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Cytotoxicity against serum stimulated mouse NIH3T3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    [PMID: 8519682]
    NIH3T3 IC50
    6 3
    Compound: Chemical probe: KN-93
    Cytotoxicity against EGF stimulated mouse NIH3T3 cells assessed as growth inhibition incubated for 72 hrs by MTT assay
    Cytotoxicity against EGF stimulated mouse NIH3T3 cells assessed as growth inhibition incubated for 72 hrs by MTT assay
    [PMID: 8519682]
    NIH3T3 IC50
    6 3
    Compound: Chemical probe: KN-93
    Cytotoxicity against FGF stimulated mouse NIH3T3 cells assessed as growth inhibition incubated for 72 hrs by MTT assay
    Cytotoxicity against FGF stimulated mouse NIH3T3 cells assessed as growth inhibition incubated for 72 hrs by MTT assay
    [PMID: 8519682]
    NIH3T3 IC50
    6 3
    Compound: Chemical probe: KN-93
    Cytotoxicity against IGF-1 stimulated mouse NIH3T3 cells assessed as growth inhibition incubated for 72 hrs by MTT assay
    Cytotoxicity against IGF-1 stimulated mouse NIH3T3 cells assessed as growth inhibition incubated for 72 hrs by MTT assay
    [PMID: 8519682]
    NIH3T3 IC50
    6 3
    Compound: Chemical probe: KN-93
    Cytotoxicity against PDGF-BB stimulated mouse NIH3T3 cells assessed as growth inhibition incubated for 72 hrs by MTT assay
    Cytotoxicity against PDGF-BB stimulated mouse NIH3T3 cells assessed as growth inhibition incubated for 72 hrs by MTT assay
    [PMID: 8519682]
    Sf9 IC50
    1.6 3
    Compound: 1, KN-93
    Inhibition of recombinant CAMK2 expressed in Sf9 cells after 20 mins
    Inhibition of recombinant CAMK2 expressed in Sf9 cells after 20 mins
    [PMID: 21292482]
    体外実験

    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].

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

    体内実験

    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].

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

    分子量

    501.04

    分子式

    C26H29ClN2O4S

    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=S(C1=CC=C(OC)C=C1)(N(C2=CC=CC=C2CN(C/C=C/C3=CC=C(Cl)C=C3)C)CCO)=O

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 50 mg/mL (99.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM 0.1996 mL 0.9979 mL 1.9958 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

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

    一般には略語で表示されます:C1V1 = C2V2

    濃度 (開始)

    C1

    ×
    体積 (開始)

    V1

    =
    濃度 (終了)

    C2

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    体積 (終了)

    V2

    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 0.83 mg/mL (1.66 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    mg/kg

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    %
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    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.42%

    参考文献
    細胞実験
    [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).

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 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
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    一般には略語で表示されます:C1V1 = C2V2

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      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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    製品名:
    KN-93
    製品番号:
    HY-15465
    数量:
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