2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. HSP
  4. KNK437

KNK437  (Synonyms: Heat Shock Protein Inhibitor I)

Cat. No.: HY-100110 Purity: 98.03%
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KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.

For research use only. We do not sell to patients.

KNK437 Chemical Structure

KNK437 Chemical Structure

CAS No. : 218924-25-5

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 92 In-stock
25 mg USD 198 In-stock
50 mg USD 370 In-stock
100 mg USD 686 In-stock
200 mg USD 924 In-stock
500 mg   Get quote  
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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 3 publication(s) in Google Scholar

KNK437 Related Antibodies

Top Publications Citing Use of Products

    KNK437 purchased from MedChemExpress. Usage Cited in: Fish Shellfish Immunol. 2017 Nov;70:185-194.  [Abstract]

    Treatment with KNK437, an antagonist of HSP27, leads to significant up-regulation of RDRP at 24 and 48 hpi.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.

    IC50 & Target[1]

    HSP105

     

    HSP70

     

    HSP40

     

    In Vitro

    KNK437 inhibits the activation of several HSPs including HSP105, HSP70, and HSP40 in COLO 320DM (human colon carcinoma) cells. KNK437 (100 μM) inhibits thermotolerance in COLO 320DM cells after the first heat treatment. KNK437 shows inhibitory effects on thermotolerance dose-dependently in COLO 320DM cells (0-200 μM) and HeLa S3 cells (100, 200 μM)[1]. KNK437 (100 μM) exhibits inhibitory activities against the methylation of H3-Lys4 before or after heat-treatment in HSC4 cells and KB cells, but does not affect that of H3 Lys9. KNK437 also suppresses the expression of HSP70[3].

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

    KNK437 Related Antibodies
    In Vivo

    KNK437 is a weakly toxic agent. KNK437 (62.5-400 mg/kg) recovers bodyweight losses of tumor-free CD-1 (ICR) mice. KNK437 (200 mg/kg) alone shows no antitumor effects and does not increase the thermosensitivity of nontolerant tumors. KNK437 improves the antitumor effects of fractionated heat treatment at 44°C at 200 mg/kg in a synergistic manner. KNK437 (200 mg/kg, i.p.) suppresses the induction of thermotolerance when administrated 6 h before the initial heating[2].

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

    245.23

    Formula

    C13H11NO4
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=CN1C(/C(CC1)=C/C2=CC=C(OCO3)C3=C2)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 31.25 mg/mL (127.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.0778 mL 20.3890 mL 40.7780 mL
    5 mM 0.8156 mL 4.0778 mL 8.1556 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.

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    • 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)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: 1.67 mg/mL (6.81 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 1.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    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.
    Purity & Documentation

    Purity: 98.03%

    COA (249 KB) HNMR (250 KB) LCMS (267 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    Heat treatments at 42°C for 90 min are performed in a CO2 incubator using 25-cm2 plastic flasks. Cells (1 × 105) are seeded in the flasks, incubated at 37°C for 48 h, and then heated by immersing the flasks in a water bath (45°C ± 0.05°C). KNK437 and quercetin are dissolved in DMSO before being added at the indicated concentrations. The final concentration of DMSO in each culture medium is 0.25% (v/v), irrespective of the concentrations of the drugs. The same concentration of DMSO is used as a control. Sodium arsenite is dissolved in PBS at a concentration of 80 mM and added to the medium. Cells are treated with 300 μM sodium arsenite at 37°C for 1.5 h, rinsed, and then incubated at 37°C for 5 h before 45°C heat challenge[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    To subject the tumors to hyperthermia, the right foot of each mouse is immersed in a water bath maintained at the desired temperature to an accuracy of ± 0.05°C. After the mouse has been anesthetized with 50 mg/kg pentobarbital sodium solution, the tumor-bearing leg is pulled down into the water bath using a special sinker (weighing ∼45 g) taped to the skin of the toe. Care is taken not to impair the blood flow in the limb. While the extended right leg is receiving local heat, the mouse is air-cooled. KNK437 is dissolved in olive oil immediately before use. The KNK437 is administered i.p. 6 h before the first heat treatment. It is used mainly at a concentration of 200 mg/kg[2].

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

    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 4.0778 mL 20.3890 mL 40.7780 mL 101.9451 mL
    5 mM 0.8156 mL 4.0778 mL 8.1556 mL 20.3890 mL
    10 mM 0.4078 mL 2.0389 mL 4.0778 mL 10.1945 mL
    15 mM 0.2719 mL 1.3593 mL 2.7185 mL 6.7963 mL
    20 mM 0.2039 mL 1.0195 mL 2.0389 mL 5.0973 mL
    25 mM 0.1631 mL 0.8156 mL 1.6311 mL 4.0778 mL
    30 mM 0.1359 mL 0.6796 mL 1.3593 mL 3.3982 mL
    40 mM 0.1019 mL 0.5097 mL 1.0195 mL 2.5486 mL
    50 mM 0.0816 mL 0.4078 mL 0.8156 mL 2.0389 mL
    60 mM 0.0680 mL 0.3398 mL 0.6796 mL 1.6991 mL
    80 mM 0.0510 mL 0.2549 mL 0.5097 mL 1.2743 mL
    100 mM 0.0408 mL 0.2039 mL 0.4078 mL 1.0195 mL
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    KNK437 Related Classifications

    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:

    KNK437218924-25-5Heat Shock Protein Inhibitor IKNK 437KNK-437HSPHeat shock proteinsInhibitorinhibitorinhibit

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