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364205 GM 6001 - CAS 142880-36-2 - Calbiochem

364205
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
142880-36-2C₂₀H₂₈N₄O₄

Products

Catalogue NumberPackaging Qty/Pack
364205-1MG Plastic ampoule 1 mg
364205-5MG Plastic ampoule 5 mg
Description
OverviewA potent, cell-permeable, broad-spectrum hydroxamic acid inhibitor of matrix metalloproteinases (MMPs); (Ki = 400 pM for MMP-1; Ki = 500 pM for MMP-2; Ki = 27 nM for MMP-3; Ki = 100 pM for MMP-8; and Ki = 200 pM for MMP-9). Prevents the release of TNF-α in vivo and in vitro and abrogates endotoxin-induced lethality in mice. A 10 mM (1 mg/257 µl) solution of GM6001 (Cat. No. 364206) in DMSO is also available.
Catalogue Number364205
Brand Family Calbiochem®
SynonymsGalardin, N-[(2R)-2-(Hydroxamidocarbonylmethyl)-4-methylpentanoyl]-L-tryptophan Methylamide
References
ReferencesSolorzano, C.C., et al. 1997. Shock 7, 427.
Galardy, R.E., et al. 1994. Ann. NY Acad. Sci. 732, 315.
Galardy, R.E., et al. 1994. Cancer Res. 54, 4715.
Galardy, R.E. 1993. Drugs Future 18, 1109.
Grobelny, D., et al. 1992. Biochemistry 31, 7152.
Product Information
CAS number142880-36-2
ATP CompetitiveN
FormOff-white solid
Hill FormulaC₂₀H₂₈N₄O₄
Chemical formulaC₂₀H₂₈N₄O₄
ReversibleN
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
ApplicationGM 6001, CAS 142880-36-2, is a potent, cell-permeable, broad-spectrum inhibitor of MMPs (Ki = 400 pM for MMP-1; 500 pM for MMP-2; 27 nM for MMP-3; 100 pM for MMP-8; and 200 pM for MMP-9).
Biological Information
Primary TargetMMP-1
Primary Target K<sub>i</sub>400 pM for MMP-1; 500 pM for MMP-2; 27 nM for MMP-3; 100 pM for MMP-8; 200 pM for MMP-9
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage -20°C
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
364205-1MG 04055977213744
364205-5MG 04055977213799

Documentation

GM 6001 - CAS 142880-36-2 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

GM 6001 - CAS 142880-36-2 - Calbiochem Certificates of Analysis

TitleLot Number
364205

References

Reference overview
Solorzano, C.C., et al. 1997. Shock 7, 427.
Galardy, R.E., et al. 1994. Ann. NY Acad. Sci. 732, 315.
Galardy, R.E., et al. 1994. Cancer Res. 54, 4715.
Galardy, R.E. 1993. Drugs Future 18, 1109.
Grobelny, D., et al. 1992. Biochemistry 31, 7152.

Citations

Title
  • K. Fredriksson, et al. (2006) Red blood cells increase secretion of matrix metalloproteinases from human lung fibroblasts in vitro. American Journal of Physiology Lung Cellular and Molecular Physiology 290, L326-L333.
  • Anthony R. White, et al. (2006) Degradation of the alzheimer disease amyloid -peptide by metal-dependent up-regulation of metalloprotease activity. journal of Biological Chemistry 281, 17670-17680.
  • IM, E., et al. 2005. Molecular Biology of the Cell 16, 3488.
  • Daniel W. Lambert, et al. (2005) Tumor Necrosis Factor- Convertase (ADAM17) Mediates Regulated Ectodomain Shedding of the Severe-acute Respiratory Syndrome-Coronavirus (SARS-CoV) Receptor, Angiotensin-converting Enzyme-2 (ACE2). Journal of Biological Chemistry 280, 30113-30119.
  • Haili Su, et al. (2005) Noninvasive targeted imaging of matrix metalloproteinase activation in a murine model of postinfarction remodeling. Circulation 112, 3157-3167.
  • Data Sheet

    Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

    Revision07-April-2008 RFH
    SynonymsGalardin, N-[(2R)-2-(Hydroxamidocarbonylmethyl)-4-methylpentanoyl]-L-tryptophan Methylamide
    DescriptionA cell-permeable, potent broad-spectrum hydroxamic acid inhibitor of matrix metalloproteinases (MMPs). [Ki = 0.4 nM for skin fibroblast collagenase (MMP-1); Ki = 0.5 nM for gelatinase A (MMP-2); Ki = 27 nM for stromelysin (MMP-3); Ki = 0.1 nM for neutrophil collagenase (MMP-8); and Ki = 0.2 nM for gelatinase B (MMP-9)]. Also prevents the release of TNF-α in vivo and in vitro and abrogates endotoxin-induced lethality in mice.
    FormOff-white solid
    CAS number142880-36-2
    Chemical formulaC₂₀H₂₈N₄O₄
    Structure formulaStructure formula
    Purity≥95% by HPLC
    SolubilityDMSO (5 mg/ml)
    Storage -20°C
    Do Not Freeze Ok to freeze
    Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
    Toxicity Standard Handling
    ReferencesSolorzano, C.C., et al. 1997. Shock 7, 427.
    Galardy, R.E., et al. 1994. Ann. NY Acad. Sci. 732, 315.
    Galardy, R.E., et al. 1994. Cancer Res. 54, 4715.
    Galardy, R.E. 1993. Drugs Future 18, 1109.
    Grobelny, D., et al. 1992. Biochemistry 31, 7152.
    Citation
  • K. Fredriksson, et al. (2006) Red blood cells increase secretion of matrix metalloproteinases from human lung fibroblasts in vitro. American Journal of Physiology Lung Cellular and Molecular Physiology 290, L326-L333.
  • Anthony R. White, et al. (2006) Degradation of the alzheimer disease amyloid -peptide by metal-dependent up-regulation of metalloprotease activity. journal of Biological Chemistry 281, 17670-17680.
  • IM, E., et al. 2005. Molecular Biology of the Cell 16, 3488.
  • Daniel W. Lambert, et al. (2005) Tumor Necrosis Factor- Convertase (ADAM17) Mediates Regulated Ectodomain Shedding of the Severe-acute Respiratory Syndrome-Coronavirus (SARS-CoV) Receptor, Angiotensin-converting Enzyme-2 (ACE2). Journal of Biological Chemistry 280, 30113-30119.
  • Haili Su, et al. (2005) Noninvasive targeted imaging of matrix metalloproteinase activation in a murine model of postinfarction remodeling. Circulation 112, 3157-3167.