Name: GM 6001
Price: 349.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    GM 6001 is a broad-spectrum inhibitor of MMP with Ki values of 0.4nM, 0.5nM, 27nM, 0.1nM and 0.2nM, respectively for MMP-1,2,3,8 and 9 [1].
    MMPs are divided into 4 subfamilies: stromelysins, gelatinases, membrane-type MMPs, and collagenases. They play major roles in mediating the effects of IL-1 during meniscal healing. As an inhibitor of MMP, GM 6001 is reported to enhance the repair of meniscal lesions in an inflammatory microenvironment. MMPs also play roles in the transactivation of EGFR induced by GPCR agonists. It is reported that treatment of GM 6001 inhibits the phosphorylation of EGFR as well as the activation of ERK induced by bombesin or LPA. The DNA synthesis induced by bombesin or LPA is also attenuated by GM 6001 since the activity of MMP is required for the GPCR-induced late response mitogenic signaling [1, 2].
    
    [1] McNulty AL, Weinberg JB, Guilak F. Inhibition of matrix metalloproteinases enhances in vitro repair of the meniscus. Clin Orthop Relat Res. 2009 Jun;467(6):1557-67.
    [2] Santiskulvong C, Rozengurt E. Galardin (GM 6001), a broad-spectrum matrix metalloproteinase inhibitor, blocks bombesin- and LPA-induced EGF receptor transactivation and DNA synthesis in rat-1 cells. Exp Cell Res. 2003 Nov 1;290(2):437-46.
- Properties
  - Alternative Name
    
    (2R)-N'-hydroxy-N-[(2S)-3-(1H-indol-3-yl)-1-(methylamino)-1-oxopropan-2-yl]-2-(2-methylpropyl)butanediamide
    
    CAS Number
    
    142880-36-2
    
    Molecular Formula
    
    C20H28N4O4
    
    Molecular Weight
    
    388.46
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥19.42 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Wenlong Zhang, Qing Zhang, et al. "Crosstalk between IL‐15Rα+ tumor‐associated macrophages and breast cancer cells reduces CD8+ T cell recruitment." Cancer Commun (Lond). 2022 Jun;42(6):536-557. PMID: 35615815
    2. Mona Nazemi. "ECM internalisation as a novel modulator of cancer cell growth/survival." The University of Sheffield. April 2021.
    3. Tan Ma, Yuan Zhou, et al. "Maternal exposure to di-n-butyl phthalate promotes the formation of testicular tight junctions through downregulation of NF-#B/COX-2/PGE2/MMP-2 in mouse offspring." Environ Sci Technol. 2020 Jul 7;54(13):8245-8258. PMID: 32525310
    4. Tewari BP, Chaunsali L, et al. "Perineuronal nets decrease membrane capacitance of peritumoral fast spiking interneurons in a model of epilepsy." Nat Commun. 2018 Nov 9;9(1):4724. PMID: 30413686
    5. Lertudomphonwanit C, Mourya R, et al. "Large-scale proteomics identifies MMP-7 as a sentinel of epithelial injury and of biliary atresia." Sci Transl Med. 2017 Nov 22;9(417). PMID: 29167395