1. Metabolic Enzyme/Protease
  2. MMP

GM6001 (Synonyms: Galardin; Ilomastat)

Cat. No.: HY-15768 Purity: 98.23%
Data Sheet SDS Handling Instructions

GM6001 is a broad spectrum matrix metalloprotease (MMP) inhibitor, with Ki of 0.4 nM, 0.5 nM, 27 nM, 3.7 nM, 0.1 nM, 0.2 nM, 3.6 nM, 13.4 nM, 0.36 nM for MMP-1/2/3/7/8/9/12/14/26, respectively.

For research use only. We do not sell to patients.
GM6001 Chemical Structure

GM6001 Chemical Structure

CAS No. : 142880-36-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $99 In-stock
5 mg $90 In-stock
10 mg $150 In-stock
50 mg $450 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

    GM6001 purchased from MCE. Usage Cited in: Nat Commun. 2017 Mar 7;8:14483.

    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

    GM6001 purchased from MCE. Usage Cited in: Am J Physiol Cell Physiol. 2017 Sep 13:ajpcell.00006.2017.

    Effects of protease inhibitor PIC, a serine protease inhibitor AEBSF and trypsin and chymotrypsin inhibitors Aprotinin (Aprot, 0.1 mM) on PRR cleavage induced by BSA in HK-2 cells.

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    • Biological Activity

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    • References

    Description

    GM6001 is a broad spectrum matrix metalloprotease (MMP) inhibitor, with Ki of 0.4 nM, 0.5 nM, 27 nM, 3.7 nM, 0.1 nM, 0.2 nM, 3.6 nM, 13.4 nM, 0.36 nM for MMP-1/2/3/7/8/9/12/14/26, respectively.

    IC50 & Target

    Ki: 0.4 nM (MMP-1), 0.5 nM (MMP-2), 27 nM (MMP-3), 3.7 nM (MMP-7), 0.1 nM (MMP-8), 0.2 nM (MMP-9), 3.6 nM (MMP-12), 13.4 nM (MMP-14), 0.36 nM (MMP-26)

    In Vitro

    GM6001 inhibits human skin fibroblast collagenase with Ki of 0.4 nM when assayed with a synthetic thio ester substrate at pH 6.5, with 50-fold selectivity over two bacterial enzymes, thermolysin and Pseudomonas aeruginosa elastase[1]. GM 6001 (0.1 nM-10 nM) inhibits gelatinase A and gelatinase B produced by T-cells, and thus inhibits T-cell homing[4]

    In Vivo

    GM6001 (400 μg/mL) prevents corneal ulceration after severe alkali injury[2]. GM6001 significantly inhibits intimal hyperplasia and intimalcollagen content, and it increases lumen area in stented arteries without effects on proliferation rates in rabbit model after stenting[3].

    References
    Preparing Stock Solutions
    Concentration Volume 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
    10 mM 0.2574 mL 1.2871 mL 2.5743 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [1]

    Collagenase assay uses the synthetic thiol ester substrate Ac-Pro-Leu-Gly-SCH(i-Bu)CO-Leu-Gly-OEt at pH 6.5. The collagenase concentration is 1-2 nM, and the substrate concentrations are from 0.1 to 0.7 nM. Km is found to vary between 1.5 and 4 mM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    GM6001 is prepared in placebo.

    To assess the effects of MMP inhibition, animals are given daily injections of either vehicle (“placebo group”) or GM6001 (100 mg/kg per day as subcutaneous suspension), beginning one day before the second injury until seven days after the procedure. 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. For biochemical studies, iliac artery tissue is removed under general anesthetic, followed by a fatal intracardiac injection of thiopentol. For histomorphometric studies, iliac arteries are perfusion-fixed in 10% buffered formalin for 20 min at a perfusion pressure of 80 mm Hg. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    388.46

    Formula

    C₂₀H₂₈N₄O₄

    CAS No.

    142880-36-2

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 47 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 98.23%

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    Inquiry Information

    Product Name:
    GM6001
    Cat. No.:
    HY-15768
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