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Inhibitor of TNF-α processing
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).
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Product Details
| Alternative Name |
IC3, N-(R)-(2-(Hydroxyaminocarbonyl)methyl)-4-methylpentanoyl-L-t-butyl-glycine-L-alanine 2-aminoethyl amide |
|---|---|
| Appearance |
Lyophilized solid. |
| Formula |
C19H37N5O5 |
| MW |
415.28 |
| Purity |
≥99% (HPLC) |
| Sequence |
(IC-3) |
| Solubility |
Soluble in water (at least 20mM) or 100% ethanol (at least 5mg/ml) |
Handling & Storage
| Use/Stability |
As indicated on product label or CoA when stored as recommended. |
|---|---|
| Long Term Storage |
-20°C |
| Shipping |
Blue Ice |
| Regulatory Status |
RUO – Research Use Only |
|---|
- 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 — Full Text
- 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 — Full Text
- 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
- TWEAK transactivation of the epidermal growth factor receptor mediates renal inflammation: S. Rayego-Mateos, et al.; J. Pathol. 231, 480 (2013), Abstract
- 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 — Full Text
- 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
- Regulated proteolysis of Trop2 drives epithelial hyperplasia and stem cell self-renewal via β-catenin signaling: Stoyanova, T., Goldstein, A. S., et al.; Genes Dev. 26, 2271 (2012), 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
- 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
- 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 — Full Text
- 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
- Function of an axonal chemoattractant modulated by metalloprotease activity: M. J. Galko, et al.; Science 289, 1365 (2000), 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
- 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
- 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
- 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
- Crystal structure of the catalytic domain of human tumor necrosis factor-alpha-converting enzyme: K. Maskos, et al.; PNAS 95, 3408 (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
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