2. Metabolic Enzyme/Protease
  3. MMP
  4. KP-457

KP-457 is a selective a disintegrin and metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than for other MMPs and ADAM10, and IC50s are 11.1 nM (ADAM17), 748 nM (ADAM10), 717 nM (MMP2), 9760 nM (MMP3), 2200 nM (MMP8), 5410 nM (MMP9), 930 nM (MMP13), 2140 nM (MMP14), and 7100 nM (MMP17), respectively.

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

CAS No. : 1365803-52-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of KP-457:

KP-457 Related Antibodies

Top Publications Citing Use of Products

    KP-457 purchased from MedChemExpress. Usage Cited in: J Thromb Haemost. 2023 Aug;21(8):2223-2235.  [Abstract]

    Relative glycocalicin levels in platelet supernatant of unstimulated platelets or after 180 minutes stimulation in absence or presence of following inhibitors; marimastat, KP-457, ADAM17 prodomain or human inhibitory anti-ADAM17 monoclonal antibody D1(A12). Glycocalicin levels are expressed relative to that of paired stimulated platelets in the absence of any inhibitor.

    KP-457 purchased from MedChemExpress. Usage Cited in: Biol Reprod. 2023 Jan 14;108(1):81-97.  [Abstract]

    KP457 (0, 5, 10, 15 μM; 1.5 h) had no significant effect on oocyte-ZP detachment even at >10 μM.

    View All MMP Isoform Specific Products:

    View All Isoforms
    MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    KP-457 is a selective a disintegrin and metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than for other MMPs and ADAM10, and IC50s are 11.1 nM (ADAM17), 748 nM (ADAM10), 717 nM (MMP2), 9760 nM (MMP3), 2200 nM (MMP8), 5410 nM (MMP9), 930 nM (MMP13), 2140 nM (MMP14), and 7100 nM (MMP17), respectively.

    IC50 & Target[1]

    ADAM17

    11.1 nM (IC50)

    ADAM10

    748 nM (IC50)

    MMP2

    717 nM (IC50)

    MMP13

    930 nM (IC50)

    MMP14

    2140 nM (IC50)

    MMP8

    2200 nM (IC50)

    MMP9

    5410 nM (IC50)

    MMP17

    7100 nM (IC50)

    MMP3

    9760 nM (IC50)

    In Vitro

    KP-457 is a selective metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than for other MMPs and ADAM10, and IC50s are 11.1 nM (ADAM17), 748 nM (ADAM10), 717 nM (MMP2), 9760 nM (MMP3), 2200 nM (MMP8), 5410 nM (MMP9), 930 nM (MMP13), 2140 nM (MMP14), and 7100 nM (MMP17), respectively. KP-457 blocks Zn2+ chelation of the catalytic domain of ADAM17. KP-457 (15 μM) retains the expression of GPIbα on iPSC-derived platelets[1].

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

    KP-457 Related Antibodies
    In Vivo

    In a thrombus formation model using immunodeficient mice after platelet transfusion, induced pluripotent stem cells (iPSCs) platelets generated with KP-457 exerts good hemostatic function[1].

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

    480.55

    Formula

    C21H24N2O7S2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CS(=O)(NCC1=CC=C(C(N(C=O)O)CS(=O)(C2=CC=C(OCC#CC)C=C2)=O)C=C1)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (260.12 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 2.0809 mL 10.4047 mL 20.8095 mL
    5 mM 0.4162 mL 2.0809 mL 4.1619 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
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    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: ≥ 2.08 mg/mL (4.33 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.33 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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

    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: 99.18%

    SDS (393 KB)

    COA (251 KB) LCMS (96 KB)

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

    Briefly, 3 × 104 hematopoietic progenitor cells (HPCs) derived from iPS-sacs on C3H10T1/2 feeder cells in the presence of 20 ng/mL vascular endothelial growth factor are transferred on day 14 of culture onto C3H10T1/2 feeder cells in differentiation medium supplemented with 50 ng/mL stem cell factor, 100 ng/mL thrombopoietin, 25 U/mL heparin sodium, and KP-457 at 24°C or 37°C. The medium is refreshed every 3 days, and nonadherent cells are collected and analyzed on days 22-24[1].

    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, 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 2.0809 mL 10.4047 mL 20.8095 mL 52.0237 mL
    5 mM 0.4162 mL 2.0809 mL 4.1619 mL 10.4047 mL
    10 mM 0.2081 mL 1.0405 mL 2.0809 mL 5.2024 mL
    15 mM 0.1387 mL 0.6936 mL 1.3873 mL 3.4682 mL
    20 mM 0.1040 mL 0.5202 mL 1.0405 mL 2.6012 mL
    25 mM 0.0832 mL 0.4162 mL 0.8324 mL 2.0809 mL
    30 mM 0.0694 mL 0.3468 mL 0.6936 mL 1.7341 mL
    40 mM 0.0520 mL 0.2601 mL 0.5202 mL 1.3006 mL
    50 mM 0.0416 mL 0.2081 mL 0.4162 mL 1.0405 mL
    60 mM 0.0347 mL 0.1734 mL 0.3468 mL 0.8671 mL
    80 mM 0.0260 mL 0.1301 mL 0.2601 mL 0.6503 mL
    100 mM 0.0208 mL 0.1040 mL 0.2081 mL 0.5202 mL
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    KP-457 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:

    KP-4571365803-52-6KP457KP 457MMPMatrix metalloproteinasesInhibitorinhibitorinhibit

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