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    Ilomastat (GM6001, Galardin)
    Ilomastat (GM6001, Galardin)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0737
    CAS #: 142880-36-2Purity ≥98%

    Description: Ilomastat (GM-6001; GM6001; Galardin), a member of the hydroxamic acid class of reversible metallopeptidase inhibitors with important biological activity, is a potent, synthetic, and broad spectrum matrix metalloprotease (MMP) inhibitor. It inhibits MMP-1/23/7/8/9/12/14/26 with Ki values 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, respectively. Ilomastat inhibits human skin fibroblast collagenase with Ki of 0.4 nM using the synthetic thiol ester substrate Ac-Pro-Leu-Gly-SCH(i-Bu)CO-Leu-Gly-OEt at pH 6.5. Topical application of Ilomastat prevented corneal ulceration after severe alkali injury and that a combination containing Ilomastat, epidermal growth factor, fibronectin, and aprotinin promoted stable regeneration of corneal epithelium after moderate alkali injury.

    References: Biochemistry. 1992 Aug 11;31(31):7152-4; Invest Ophthalmol Vis Sci. 1992 Nov;33(12):3325-31; J Am Coll Cardiol. 2002 Jun 5;39(11):1852-8.

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    Molecular Weight (MW)388.46
    FormulaC20H28N4O4
    CAS No.142880-36-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 78 mg/mL (200.8 mM)
    Water: <1 mg/mL
    Ethanol: 8 mg/mL (20.6 mM)
    SMILES CodeO=C(NC)[[email protected]@H](NC([[email protected]@H](CC(NO)=O)CC(C)C)=O)CC1=CNC2=CC=CC=C21
    SynonymsIlomastat; GM6001; galardin; GM-6001; GM 6001 

    Chemical Name: (R)-N1-((S)-3-(1H-indol-3-yl)-1-(methylamino)-1-oxopropan-2-yl)-N4-hydroxy-2-isobutylsuccinamide

    SMILES Code: O=C(NC)[[email protected]@H](NC([[email protected]@H](CC(NO)=O)CC(C)C)=O)CC1=CNC2=CC=CC=C21


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    In Vitro

    In vitro activity: Ilomastat (also known as GM6001 or Galardin) is a member of the hydroxamic acid class of reversible metallopeptidase inhibitors, it is a potent, synthetic, and broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26 with Ki values 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, respectively. Ilomastat inhibits human skin fibroblast collagenase with Ki of 0.4 nM using the synthetic thiol ester substrate Ac-Pro-Leu-Gly-SCH(i-Bu)CO-Leu-Gly-OEt at pH 6.5. Topical application of Ilomastat prevented corneal ulceration after severe alkali injury and that a combination containing Ilomastat, epidermal growth factor, fibronectin, and aprotinin promoted stable regeneration of corneal epithelium after moderate alkali injury. 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. GM 6001 (0.1 nM - 10 nM) inhibits gelatinase A and gelatinase B produced by T-cells, thus inhibits T-cell homing.


    Kinase Assay: 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. 


    Cell Assay: In MDA-MB-435 cells, GM 6001 increases the respiratory rate by 80% and [3H] thymidine incorporation by 50% when treated for 6 h and 12 h respectively, which suggest that GM 6001 increase DNA synthesis. GM 6001 also increases ERK activity and p38 kinase activity.

    In VivoTopical application of GM6001 (400 μg/ml) prevents corneal ulceration after severe alkali injury. In rabbit model after stenting, GM6001 significantly inhibits intimal hyperplasia and intimalcollagen content, and it increases lumen area in stented arteries without effects on proliferation rates.
    Animal modelRabbit
    Formulation & DosageDissolved in 50 mM HEPES buffer; 100 mg/kg; s.c. injection
    ReferencesBiochemistry. 1992 Aug 11;31(31):7152-4; Invest Ophthalmol Vis Sci. 1992 Nov;33(12):3325-31; J Am Coll Cardiol. 2002 Jun 5;39(11):1852-8.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     

    Ilomastat (GM6001, Galardin)

    Collagen content in the intima (left) and media/adventitia (right). J Am Coll Cardiol. 2002 Jun 5;39(11):1852-8.
     

    Ilomastat (GM6001, Galardin)

    Gelatin zymogram in balloon angioplasty (BA)-treated and stent arteries. J Am Coll Cardiol. 2002 Jun 5;39(11):1852-8.
     

    Ilomastat (GM6001, Galardin)

    Collagen synthesis in cultured smooth muscle cells showed a dose-related inhibition with GM6001. J Am Coll Cardiol. 2002 Jun 5;39(11):1852-8.
     

    Ilomastat (GM6001, Galardin)

    Representative photomicrograph of elastic trichrome-stained cross sections of stented arteries showing increased intimal hyerplasia in a placebo-treated artery (A) compared to a GM6001-treated animal (B). J Am Coll Cardiol. 2002 Jun 5;39(11):1852-8.
     

    Ilomastat (GM6001, Galardin)

    Intimal cross-sectional area (CSA) (A), lumen CSA (B) and intimal collagen content (C) at 10 weeks in stented arteries after treatment with GM6001 or placebo. J Am Coll Cardiol. 2002 Jun 5;39(11):1852-8.
     

    Ilomastat (GM6001, Galardin)

    Schematic diagram outlining study protocol. BA = balloon angioplasty; MMP = matrix metalloproteinase.


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