GM 6001

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2983/10
GM 6001 | CAS No. 142880-36-2 | Synthetic Metalloprotease Inhibitors
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Description: Broad spectrum MMP inhibitor
Alternative Names: Galardin,Ilomastat

Chemical Name: (2R)-N4-Hydroxy-N1-[(1S)-1-(1H-indol-3-ylmethyl)-2-(methylamino)-2-oxoethyl]-2-(2-methylpropyl)butanediamide

Purity: ≥95%

Product Details
Citations (10)
Reviews

Biological Activity

GM 6001 is a broad spectrum MMP inhibitor. Reduces infarct volume following middle cerebral artery occlusion in an ischemic mouse model. Also inhibits human skin fibroblast collagenase (Ki = 0.4 nM).

Technical Data

M.Wt:
388.46
Formula:
C20H28N4O4
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥95%
Storage:
Store at -20°C
CAS No:
142880-36-2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. ErbB4 signaling stimulates pro-inflammatory macrophage apoptosis and limits colonic inflammation
    MA Schumacher, M Hedl, C Abraham, JK Bernard, PR Lozano, JJ Hsieh, D Almohazey, EB Bucar, S Punit, PJ Dempsey, MR Frey
    Cell Death Dis, 2017;8(2):e2622.
  2. Up-Regulated Expression of Matrix Metalloproteinases in Endothelial Cells Mediates Platelet Microvesicle-Induced Angiogenesis
    C Sun, SB Feng, ZW Cao, JJ Bei, Q Chen, WB Zhao, XJ Xu, Z Zhou, ZP Yu, HY Hu
    Cell. Physiol. Biochem., 2017;41(6):2319-2332.
  3. Dermatan sulfate is a player in the transglutaminase 2 interaction network
    G Wisowski, EM Ko?ma, T Bielecki, A Pude?ko, K Olczyk
    PLoS ONE, 2017;12(2):e0172263.
  4. Signaling pathways induced by serine proteases to increase intestinal epithelial barrier function
    KA Lahey, NJ Ronaghan, J Shang, SP Dion, A Désilets, R Leduc, WK MacNaughto
    PLoS ONE, 2017;12(7):e0180259.
  5. Modulation of proteoglycan receptor PTP? enhances MMP-2 activity to promote recovery from multiple sclerosis
    F Luo, AP Tran, L Xin, C Sanapala, BT Lang, J Silver, Y Yang
    Nat Commun, 2018;9(1):4126.
  6. TREM2 shedding by cleavage at the H157-S158 bond is accelerated for the Alzheimer's disease-associated H157Y variant
    P Thornton, J Sevalle, MJ Deery, G Fraser, Y Zhou, S Ståhl, EH Franssen, RB Dodd, S Qamar, B Gomez Pere, LS Nicol, S Eketjäll, J Revell, C Jones, A Billinton, PH St George-, I Chessell, DC Crowther
    EMBO Mol Med, 2017;0(0):.
  7. Involvement of matrix metalloproteinase-mediated proteolysis of neural cell adhesion molecule in the development of cerebral ischemic neuronal damage.
    Shichi et al.
    J.Pharmacol.Exp.Ther., 2011;338:701
  8. Inhibition of skin fibroblast Col., thermolysin, and Pseudomonas aeruginosa elastase by peptide hydroxamic acids.
    Grobelny et al.
    Biochemistry, 1992;31:7152
  9. Leptin stimulates endothelin-1 expression via extracellular signal-regulated kinase by epidermal growth factor receptor transactivation in rat aortic smooth muscle cells.
    Chao et al.
    Eur.J.Pharmacol., 2007;573:49

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Citations for GM 6001

The citations listed below are publications that use Tocris products. Selected citations for GM 6001 include:

10 Citations: Showing 1 - 10

  1. Myh10 deficiency leads to defective extracellular matrix remodeling and pulmonary disease.
    Authors: Kim Et al.
    Nat Commun  2018;9:4600
  2. Modulation of proteoglycan receptor PTPσ enhances MMP-2 activity to promote recovery from multiple sclerosis.
    Authors: Luo Et al.
    Nat Commun  2018;9:4126
  3. ErbB4 signaling stimulates pro-inflammatory macrophage apoptosis and limits colonic inflammation.
    Authors: Schumacher
    Cell Death Dis  2017;8:e2622
  4. Up-Regulated Expression of Matrix Metalloproteinases in Endothelial Cells Mediates Platelet Microvesicle-Induced Angiogenesis.
    Authors: Sun Et al.
    Cell Physiol Biochem  2017;41:2319
  5. Matrix metalloproteinase activity stimulates N-cadherin shedding and the soluble N-cadherin ectodomain promotes classical microglial activation.
    Authors: Conant Et al.
    J Neuroinflammation  2017;14:56
  6. Signaling pathways induced by serine proteases to increase intestinal epithelial barrier function.
    Authors: Lahey Et al.
    PLoS One  2017;12:e0180259
  7. TGFβ loss activates ADAMTS-1-mediated EGF-dependent invasion in a model of esophageal cell invasion.
    Authors: Bras Et al.
    PLoS One  2015;330:29
  8. PRL-3 mediates the protein maturation of ULBP2 by regulating the tyrosine phosphorylation of HSP60.
    Authors: Leung Et al.
    J Immunol  2015;194:2930
  9. CD40-TRAF Signaling Upregulates CX3CL1 and TNF-α in Human Aortic Endothelial Cells but Not in Retinal Endothelial Cells.
    Authors: Greene Et al.
    Proc Natl Acad Sci U S A  2015;10:e0144133
  10. STAT induce Ins-degrading enzyme secretion from astrocytes via an autophagy-based unconventional secretory pathway.
    Authors: Son Et al.
    Mol Neurodegener  2015;10:56

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