1. Metabolic Enzyme/Protease Apoptosis
  2. Proteasome Apoptosis
  3. K-7174

K-7174 is an orally active proteasome and GATA inhibitor. K-7174 is a cell adhesion inhibitor. K-7174 induces cell apoptosis. K-7174 shows antitumor activities, it can be used for the research of cancer.

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

K-7174 Chemical Structure

K-7174 Chemical Structure

CAS No. : 191089-59-5

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5 mg USD 80 In-stock
10 mg USD 130 In-stock
25 mg USD 260 In-stock
50 mg USD 420 In-stock
100 mg USD 650 In-stock
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Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of K-7174:

Top Publications Citing Use of Products

    K-7174 purchased from MedChemExpress. Usage Cited in: Brain Res. 2022.

    K-7174 (30 mg/kg; i.p.; 3 times a week for 6 weeks) improves lupus-like symptoms in MRL/lpr mice. The deposition of IgG and C3 in the kidneys of mice in the MRL/lpr group is significantly higher than that in the control group, but K-7174 can significantly inhibit this deposition.

    K-7174 purchased from MedChemExpress. Usage Cited in: Brain Res. 2022.

    K-7174 significantly increases the protein and gene levels of ZO1 and Occludin in NPSLE model mouse (MRL/lpr mice) brain.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    K-7174 is an orally active proteasome and GATA inhibitor. K-7174 is a cell adhesion inhibitor. K-7174 induces cell apoptosis. K-7174 shows antitumor activities, it can be used for the research of cancer[1][2][3].

    In Vitro

    K-7174 (10 μM; 1 h) inhibits the adhesion by VCAM-1 and its ligand[1].
    K-7174 (1-30 μM; 1 h) dose-dependently suppresses the VCAM-1 expression with an IC50 value of 14 μM[1].
    K-7174 (1-30 μM; 1 h) dose-dependently suppresses the induction of VCAM-1 mRNA by TNFα with an IC50 value of 9 μM[1].
    K-7174 (10-20 μM; 24 h) dose-dependently rescues Epo production by Hep3B cells[2].
    K-7174 (2.5-30 μM; 24 h) inhibits the binding activity of GATA[2].
    K-7174 (0-25 μM; 72 h) inhibits MM cells growth and induces cell apoptosis[3].

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

    Cell Viability Assay[3]

    Cell Line: KMS12-BM, U266, and RPMI8226 cell lines
    Concentration: 0-25 μM
    Incubation Time: 72 h
    Result: Inhibited MM cells growth.

    Apoptosis Analysis[3]

    Cell Line: KMS12-BM, U266, and RPMI8226 cell lines
    Concentration: 10 μM
    Incubation Time: 48 h
    Result: Significantly increased apoptosis of MM cells with the increasing percentage of annexin-V-positive cells.
    In Vivo

    K-7174 (30 mg/kg; i.p. once daily for 9 days) reverses the decreasing of hemoglobin concentrations and reticulocyte counts by IL-1β or TNF-α[2].
    K-7174 (75 mg/kg; i.p. once daily for 14 days) inhibits the tumor growth in vivo[3].
    K-7174 (50 mg/kg; p.o. once daily for 14 days) inhibits the tumor growth in vivo and shows a better effect than intraperitoneal injection[3].

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

    Animal Model: ICR mice with IL-β or TNF-α injection[2]
    Dosage: 30 mg/kg
    Administration: Intraperitoneal injection; 30 mg/kg once daily for 9 days
    Result: Increased erythropoietin (Epo) production, reticulocyte counts, and hemoglobin (Hb) concentrations
    Animal Model: NOD/SCID mice with murine xenograft[3]
    Dosage: 75 mg/kg
    Administration: Intraperitoneal injection; once daily for 14 days
    Result: Significantly decreased tumor volume, but showed a significant body weight reduction after 10 days.
    Animal Model: NOD/SCID mice with murine xenograft[3]
    Dosage: 50 mg/kg
    Administration: Oral gavage; once daily for 14 days
    Result: Showed an anti-myeloma activity. Proved oral administration is more effective than intraperitoneal injection.
    Molecular Weight

    568.74

    Formula

    C33H48N2O6

    CAS No.
    Appearance

    Oil

    Color

    Colorless to light yellow

    SMILES

    COC1=C(OC)C(OC)=CC(/C=C/CCCN2CCN(CCC/C=C/C3=CC(OC)=C(OC)C(OC)=C3)CCC2)=C1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Pure form -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (175.83 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 1.7583 mL 8.7914 mL 17.5827 mL
    5 mM 0.3517 mL 1.7583 mL 3.5165 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    V2

    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: ≥ 5 mg/mL (8.79 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 5 mg/mL (8.79 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (per animal)

    g

    Dosing volume
    (per animal)

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    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
    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7583 mL 8.7914 mL 17.5827 mL 43.9568 mL
    5 mM 0.3517 mL 1.7583 mL 3.5165 mL 8.7914 mL
    10 mM 0.1758 mL 0.8791 mL 1.7583 mL 4.3957 mL
    15 mM 0.1172 mL 0.5861 mL 1.1722 mL 2.9305 mL
    20 mM 0.0879 mL 0.4396 mL 0.8791 mL 2.1978 mL
    25 mM 0.0703 mL 0.3517 mL 0.7033 mL 1.7583 mL
    30 mM 0.0586 mL 0.2930 mL 0.5861 mL 1.4652 mL
    40 mM 0.0440 mL 0.2198 mL 0.4396 mL 1.0989 mL
    50 mM 0.0352 mL 0.1758 mL 0.3517 mL 0.8791 mL
    60 mM 0.0293 mL 0.1465 mL 0.2930 mL 0.7326 mL
    80 mM 0.0220 mL 0.1099 mL 0.2198 mL 0.5495 mL
    100 mM 0.0176 mL 0.0879 mL 0.1758 mL 0.4396 mL
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    • 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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    Cat. No.:
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