CC1100 | GM6001 MMP Inhibitor Powder

CC1100
10  mg
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      Overview

      Description
      Catalogue Number CC1100
      Brand Family Chemicon®
      Trade Name
      • Chemicon
      Description GM6001 MMP Inhibitor Powder
      Overview specificity:GM6001 MMP inhibitor, also known as Ilomastat or N-[(2R)-2-(hydroxamidocarbonylmethyl)-4-methylpentanoyl]-L-tryptophan methylamide, is a potent inhibitor of collagenases. Molecular weight: 388.47

      Reported Ki values are as follows (see Galardy Ref):

      Human MMP-1 (Fibroblast collagenase): 0.4 nM

      Human MMP-3 (Stromelysin): 27 nM

      Human MMP-2 (72 kDa gelatinase): 0.5 nM

      Human MMP-8 (Neutrophil collagenase): 0.1 nM

      Human MMP-9 (92 kDa gelatinase): 0.2 nM

      Typical working dilution for use in cultured cells is 10-25 μM. {1mg/ml solution in DMSO equals 2.57 mM}. GM6001 will precipitate from aqueous solutions exceeding 100μM. Aqueous dilutions should be performed using low salt buffers to prevent precipitation of GM6001 from solution (Recommended dilution buffer: 50 mM Tris pH7.5, 150 mM NaCl, and 20 mM CaCl2.2H20). It is recommended that the concentration of GM6001 in aqueous working solutions is determined upon dilution and confirmed prior to each use. Additional Application information:
      Use in vivo
      Typical dosage for GM6001 in animals is 50-100mg/kg body weight. It is generally administered IP every day or every other day. It is thought to cross the blood brain barrier since studies have shown it effectiveness in MS models.

      If delivered by I.V. the half life in an animal is approximate an hour so it will have to be administered quite often. Thus the preferred way is to deliver the drug by I.P as a suspension in water or saline. The half life does not change but because it is dissolving in the animal's system slowly, administration is not done as frequently. It has to be redelivered every other day or so. It can also be delivered subcutaneously in a saline suspension. The drug will precipitate as stay as a mass within the tissue, but surprisingly enough does get into the animal system to be effective.

      Solubility
      Soluble up to at least 400 mg/mL in DMSO. It can then be diluted in water and must be mixed very quickly to avoid precipitation.

      Stability
      At a concentration of 1mM (0.1mM is preferred), GM6001 decomposes at the rate of 1% per month at 4°C. At 37°C this increases to 1% per day. At -20°C it is quite stable, and as a solid very highly stable
      Low salt buffers are recommended as diluents to reduce precipitation. Diluted solutions should never be frozen.

      Concentration of the stock solution should be periodically determined by absorbance at 280 nm.
      References
      Product Information
      Presentation Lyophilized, reconstitute in DMSO (1-5 mg/ml). Other organic solvents (ethanol) have also been used (Galardy et al., 1994).
      Applications
      Application The GM6001 MMP Inhibitor Powder controls the biological activity of MMP. This small molecule/inhibitor is primarily used for Biochemicals applications.
      Key Applications
      • Inhibits Activity/Function
      Biological Information
      Purity >95% pure by HPLC; some batches can be brown when hydrated; brown color does not influence inhibition ability; in solution GM6001 ranges from clear to brown.
      Entrez Gene Number
      Entrez Gene Summary Proteins of the matrix metalloproteinase (MMP) family are involved in the breakdown of extracellular matrix in normal physiological processes, such as embryonic development, reproduction, and tissue remodeling, as well as in disease processes, such as arthritis and metastasis. Most MMP's are secreted as inactive proproteins which are activated when cleaved by extracellular proteinases. However, the enzyme encoded by this gene is stored in secondary granules within neutrophils and is activated by autolytic cleavage. Its function is degradation of type I, II and III collagens. The gene is part of a cluster of MMP genes which localize to chromosome 11q22.3.
      Gene Symbol
      • 27 kDa interstitial collagenase].
      • MMP1
      • CLG
      • MMP-1
      • CLGN
      • EC 3.4.24.7 [Contains: 22 kDa interstitial collagenase
      UniProt Number
      UniProt Summary FUNCTION: SwissProt: P22894 # Can degrade fibrillar type I, II, and III collagens.
      COFACTOR: Binds 3 calcium ions per subunit. & Binds 2 zinc ions per subunit.
      SIZE: 467 amino acids; 53412 Da
      SUBCELLULAR LOCATION: Cytoplasmic granule. Note=Stored in intracellular granules.
      TISSUE SPECIFICITY: Neutrophils.
      DOMAIN: SwissProt: P22894 The conserved cysteine present in the cysteine-switch motif binds the catalytic zinc ion, thus inhibiting the enzyme. The dissociation of the cysteine from the zinc ion upon the activation-peptide release activates the enzyme.
      SIMILARITY: Belongs to the peptidase M10A family. & Contains 4 hemopexin-like domains.
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Usage Statement
      • Unless otherwise stated in our catalog or other company documentation accompanying the product(s), our products are intended for research use only and are not to be used for any other purpose, which includes but is not limited to, unauthorized commercial uses, in vitro diagnostic uses, ex vivo or in vivo therapeutic uses or any type of consumption or application to humans or animals.
      Storage and Shipping Information
      Storage Conditions Maintain lyophilized form at 2-8º C for up to one year from date of receipt. If reconstitution is in DMSO, material is soluble to at least 400 mg/mL and storage is recommended in usable aliquots at -20 º C. Avoid repeated freeze/thaw cycles. If reconstituting in aqueous solution, store short term in undiluted aliquots at 2-8º C. See stability information for further detail.
      Packaging Information
      Qty/Pck 10 mg
      Material Size 10
      Material Package mg
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Certificates of Analysis

      TitleLot Number
      GM6001 [Ilomastat] MMP Inhibitor 2483227
      GM6001 [Ilomastat] MMP Inhibitor Powder form - 2392239 2392239
      GM6001 [Ilomastat] MMP Inhibitor Powder form - 2459006 2459006
      Millipore - COA - GM6001 [Ilomastat] MMP Inhibitor Powder form - 2070800 2070800

      References

      Reference overviewPub Med ID
      Tissue inhibitor of metalloproteinases-1 stimulates gene expression in MDA-MB-435 human breast cancer cells by means of its ability to inhibit metalloproteinases.
      Joseph F Porter,Shashi Sharma,Donna L Wilson,Maya A Kappil,Ronald P Hart,David T Denhardt
      Breast cancer research and treatment 94 2005

      Show Abstract
      16142437
      Repair of bone defects using synthetic mimetics of collagenous extracellular matrices.
      Lutolf, Matthias P, et al.
      Nat. Biotechnol., 21: 513-8 (2003) 2003

      Show Abstract
      12704396
      A null mutation for tissue inhibitor of metalloproteinases-3 (Timp-3) impairs murine bronchiole branching morphogenesis
      Gill, Sean E, et al
      Dev Biol, 261:313-23 (2003) 2003

      14499643
      Matrix metalloproteinase inhibitors: a structure-activity study.
      Levy, D E, et al.
      J. Med. Chem., 41: 199-223 (1998) 1998

      Show Abstract
      9457244
      Low molecular weight inhibitors in corneal ulceration.
      Galardy, R E, et al.
      Ann. N. Y. Acad. Sci., 732: 315-23 (1994) 1994

      7978801

      Technical Info and Required Licenses

      Title
      Fluorescent Gelatin Degradation Assays for Investigating Invadopodia Formation

      Data Sheet

      Title
      GM6001 [Ilomastat] MMP Inhibitor Powder form

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