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

364205
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₀H₂₈N₄O₄ 142880-36-2

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      364205-1MG
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          Plastic ampoule 1 mg
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          364205-5MG
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              Plastic ampoule 5 mg
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              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
              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

              Documentation

              SDS

              Title

              Safety Data Sheet (SDS) 

              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.