Inhibitor of TACE, other ADAMs, ACE secretase and other metalloproteinases. Blocks release of TNFα, TGF-α, DCC, APP, L-selectin, ACE, IL6R, NOTCH, and erbB2/HER2. Has been used in culture (typical concentration 5-100µM).
Product Details
| Alternative Name: | IC3, N-(R)-(2-(Hydroxyaminocarbonyl)methyl)-4-methylpentanoyl-L-t-butyl-glycine-L-alanine 2-aminoethyl amide |
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| Sequence: | (IC-3)
N-(R)-(2-(Hydroxyaminocarbonyl)methyl)-4-methylpentanoyl-L-t-butyl-glycine-L-alanine 2-aminoethyl amide |
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| Formula: | C19H37N5O5 |
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| MW: | 415.28 |
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| Purity: | ≥99% (HPLC) |
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| Appearance: | Lyophilized solid. |
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| Solubility: | Soluble in water (at least 20mM) or 100% ethanol (at least 5mg/ml) |
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| Shipping: | Blue Ice |
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| Long Term Storage: | -20°C |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
ADAM10 Cell Surface Expression but Not Activity Is Critical for Staphylococcus aureus a-Hemolysin-Mediated Activation of the NLRP3 Inflammasome in Human Monocytes: E.A. Ezekwe Jr., et al.; Toxins (Basel)
8, 95 (2016),
Abstract;
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Angiotensin II induced proteolytic cleavage of myocardial ACE2 is mediated by TACE/ADAM-17: a positive feedback mechanism in the RAS: V.B. Patel, et al.; J. Mol. Cell. Cardiol.
66, 167 (2014),
Abstract;
Elevated serum CXCL16 is an independent predictor of poor survival in ovarian cancer and may reflect pro-metastatic ADAM protease activity: M.J. Gooden, et al.; Br. J. Cancer
110, 1535 (2014),
Abstract;
PKCδ and θ possibly mediate FSH-induced mouse oocyte maturation via NOX-ROS-TACE cascade signaling pathway: Q. Chen, et al.; PLoS One
9, e111423 (2014),
Application(s): Cell culture medium in primary mouse cumulus-oocyte complexes,
Abstract;
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IL-7 and IL-15 instruct the generation of human memory stem T cells from naive precursors: N. Cieri, et al.; Blood
121, 573 (2013),
Abstract;
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Neutrophil apoptosis is associated with loss of signal regulatory protein alpha (SIRPα) from the cell surface: A. Stenberg, et al.; J. Leukoc. Biol.
93, 403 (2013),
Abstract;
TWEAK transactivation of the epidermal growth factor receptor mediates renal inflammation: S. Rayego-Mateos, et al.; J. Pathol.
231, 480 (2013),
Abstract;
Paracrine regulation of growth factor signaling by shed leucine-rich repeats and immunoglobulin-like domains 1: W. Yi, et al.; Exp. Cell. Res.
317, 504 (2011),
Abstract;
Epidermal growth factor and perlecan fragments produced by apoptotic endothelial cells co-ordinately activate ERK1/2-dependent antiapoptotic pathways in mesenchymal stem cells: M. Soulez, et al.; Stem Cells
28, 810 (2010),
Abstract;
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TGFβ induces proHB-EGF shedding and EGFR transactivation through ADAM activation in gastric cancer cells: M. Ebi, et al.; Biochem. Biophys. Res. Commun.
402, 449 (2010),
Abstract;
Fluorescent substrates for the proteinases ADAM17, ADAM10, ADAM8, and ADAM12 useful for high-throughput inhibitor screening: M. L. Moss, et al.; Anal. Biochem.
366, 144 (2007),
Abstract;
Transmembrane collagen XVII, an epithelial adhesion protein, is shed from the cell surface by ADAMs: C.W. Franzke, et al.; EMBO J.
21, 5026 (2002),
Abstract;
A novel proteolytic cleavage involved in Notch signaling: the role of the disintegrin-metalloprotease TACE: C. Brou, et al.; Mol. Cell
5, 207 (2000),
Abstract;
Function of an axonal chemoattractant modulated by metalloprotease activity: M. J. Galko, et al.; Science
289, 1365 (2000),
Abstract;
Cleavage of the HER2 ectodomain is a pervanadate-activable process that is inhibited by the tissue inhibitor of metalloproteases-1 in breast cancer : J. Codony-Servat, et al.; Cancer Res.
59, 1196 (1999),
Abstract;
Unaltered cleavage and secretion of angiotensin-converting enzyme in tumor necrosis factor-alpha-converting enzyme-deficient mice: R. Sadhukhan, et al.; J. Biol. Chem.
274, 10511 (1999),
Abstract;
Crystal structure of the catalytic domain of human tumor necrosis factor-alpha-converting enzyme: K. Maskos, et al.; PNAS
95, 3408 (1998),
Abstract;
Evidence that tumor necrosis factor alpha converting enzyme is involved in regulated alpha-secretase cleavage of the Alzheimer amyloid protein precursor: J. D. Buxaum, et al.; J. Biol. Chem.
273, 27765 (1998),
Abstract;
TNFalpha processing enzyme inhibitors prevent aspirin-induced TNFalpha release and protect against gastric mucosal injury in rats: S. Fioruci, et al.; Aliment. Pharmacol. Ther.
12, 1139 (1998),
Abstract;
A metalloproteinase disintegrin that releases tumour-necrosis factor-alpha from cells: R. A. Black, et al.; Nature
385, 729 (1997),
Abstract;
Angiotensin-converting enzyme secretase is inhibited by zinc metalloprotease inhibitors and requires its substrate to be inserted in a lipid bilayer: S. Parvathy, et al.; Biochem. J.
327, 37 (1997),
Abstract;
Diverse cell surface protein ectodomains are shed by a system sensitive to metalloprotease inhibitors: J. Arribas, et al.; J. Biol. Chem.
271, 11376 (1996),
Abstract;
