2. Metabolic Enzyme/Protease
  3. MMP
  4. Ilomastat

Ilomastat  (Synonyms: GM6001; Galardin)

Cat. No.: HY-15768 Purity: 98.39%
COA Handling Instructions

Molarity Calculator

Ilomastat (GM6001) is a potent and broad spectrum matrix metalloprotease (MMP) inhibitor, inhibits MMPs (IC50s, 1.5 nM for MMP-1; 1.1 nM for MMP-2; 1.9 nM for MMP-3; 0.5 nM for MMP-9), with a Ki of 0.4 nM for human skin fibroblast collagenase (MMP-1).

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

Ilomastat Chemical Structure

Ilomastat Chemical Structure

CAS No. : 142880-36-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 131 In-stock
Solution
10 mM * 1 mL in DMSO USD 131 In-stock
Solid
1 mg USD 48 In-stock
5 mg USD 119 In-stock
10 mg USD 198 In-stock
50 mg USD 594 In-stock
100 mg   Get quote  
200 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 43 publication(s) in Google Scholar

Ilomastat Related Antibodies

Top Publications Citing Use of Products

40 Publications Citing Use of MCE Ilomastat

WB
Proliferation Assay
IF

    Ilomastat purchased from MedChemExpress. Usage Cited in: Int J Nanomedicine. 2018 Aug 13;13:4641-4659.  [Abstract]

    Cellular uptake of P123-Cou6 and PG-SG-Cou6 micelles in MCF7 and MCF7/ADR cells in the presence of GM6001.

    Ilomastat purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Mar 25;498(1):125-131.  [Abstract]

    Cell lysates are immunoblotted with antibodies against Claudin-4, E-cadherin, β-catenin, MMP9 and GAPDH.

    Ilomastat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2017 Mar 7;8:14483.  [Abstract]

    A transwell assay is performed in MDA-MB-231 cells, GM6001-treated MDA-MB-231 cells or GM6001-treated and CRISPR/Cas9-mediated VCL deleted MDA-MB-231 cells

    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

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Ilomastat (GM6001) is a potent and broad spectrum matrix metalloprotease (MMP) inhibitor, inhibits MMPs (IC50s, 1.5 nM for MMP-1; 1.1 nM for MMP-2; 1.9 nM for MMP-3; 0.5 nM for MMP-9), with a Ki of 0.4 nM for human skin fibroblast collagenase (MMP-1).

    IC50 & Target[1][5]

    MMP-9

    0.5 nM (IC50)

    MMP-2

    1.1 nM (IC50)

    MMP-1

    1.5 nM (IC50)

    MMP-3

    1.9 nM (IC50)

    Fibroblast collagenase

    0.4 nM (Ki, Human skin)

    Thermolysin

    20 nM (Ki)

    Eastase

    20 nM (Ki)

    In Vitro

    Ilomastat (GM6001) inhibits human skin fibroblast collagenase, thermolysin and elastase with Kis of 0.4 nM, 20 nM, 20 nM, resepctively[1]. Ilomastat (0.1-10 nM) inhibits gelatinase A and gelatinase B produced by T-cells. Ilomastat inhibits T-cell homing[4].

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

    Ilomastat Related Antibodies
    In Vivo

    Ilomastat (GM6001) (400 μg/mL) inhibits corneal ulceration after severe alkali injury in animals[2]. Ilomastat (GM6001) significantly suppresses intimal hyperplasia and intimalcollagen content. Ilomastat increases lumen area in stented arteries, shows no activity on proliferation rates in rabbit model after stenting[3].

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

    388.46

    Formula

    C20H28N4O4
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=C(N[C@@H](CC1=CNC2=C1C=CC=C2)C(NC)=O)[C@H](CC(C)C)CC(NO)=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 : ≥ 47 mg/mL (120.99 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5743 mL 12.8713 mL 25.7427 mL
    5 mM 0.5149 mL 2.5743 mL 5.1485 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)

    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: ≥ 2.5 mg/mL (6.44 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.44 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  0.5% CMC-Na/saline water

      Solubility: 10 mg/mL (25.74 mM); Suspended solution; Need ultrasonic

    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: 98.39%

    COA (255 KB) LCMS (87 KB)

    Handling Instructions (2659 KB)
    References
    Animal Administration
    [3]

    To assess the effects of MMP inhibition, animals are given daily injections of either vehicle (“placebo group”) or Ilomastat (GM6001) (100 mg/kg per day as subcutaneous suspension), beginning one day before the second injury until seven days after the procedure. Ilomastat (GM6001) is a nonspecific hydroxamic acid-based MMPI with potent inhibitory activity against collagenase, gelatinases and stromelysin. Animals are euthanized at either 1 week or 10 weeks after the second injury.

    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 2.5743 mL 12.8713 mL 25.7427 mL 64.3567 mL
    5 mM 0.5149 mL 2.5743 mL 5.1485 mL 12.8713 mL
    10 mM 0.2574 mL 1.2871 mL 2.5743 mL 6.4357 mL
    15 mM 0.1716 mL 0.8581 mL 1.7162 mL 4.2904 mL
    20 mM 0.1287 mL 0.6436 mL 1.2871 mL 3.2178 mL
    25 mM 0.1030 mL 0.5149 mL 1.0297 mL 2.5743 mL
    30 mM 0.0858 mL 0.4290 mL 0.8581 mL 2.1452 mL
    40 mM 0.0644 mL 0.3218 mL 0.6436 mL 1.6089 mL
    50 mM 0.0515 mL 0.2574 mL 0.5149 mL 1.2871 mL
    60 mM 0.0429 mL 0.2145 mL 0.4290 mL 1.0726 mL
    80 mM 0.0322 mL 0.1609 mL 0.3218 mL 0.8045 mL
    100 mM 0.0257 mL 0.1287 mL 0.2574 mL 0.6436 mL
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    Ilomastat 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:

    Ilomastat142880-36-2GM6001 GalardinGM 6001GM-6001MMPMatrix metalloproteinasesInhibitorinhibitorinhibit

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