GI 254023X
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Description: Selective ADAM10 metalloprotease inhibitor
Chemical Name: (2R)-N-[(1S)-2,2-Dimethyl-1-[(methylamino)carbonyl]propyl]-2-[(1S)-1-(N-hydroxyformamido)ethyl]-5-phenylpentanamide
Purity: ≥98%
Biological Activity
GI 254023X is a selective ADAM10 metalloprotease inhibitor; displays over 100-fold higher potency at ADAM10 compared to ADAM17. Blocks constitutive release of IL-6R, CX3CL1 and CXCL16 in cell-based cleavage experiments. Inhibits calcium ionophore-induced betacellulin shedding in IMPE cells. Prevents E-cadherin cleavage in A549 cells. Inhibits ADAM10 mediated neuronal outgrowth of dorsal root ganglion neurons in vitro.Technical Data
M.Wt:
391.5
Formula:
C21H33N3O4
Solubility:
Soluble to 20 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
260264-93-5
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.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline.
Background References
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The ADAM10 prodomain is a specific inhibitor of ADAM10 proteolytic activity and inhibits cellular shedding events.
Moss ML, Bomar M, Liu Q, Sage H, Dempsey P, Lenhart PM, Gillispie PA, Stoeck A, Wildeboer D, Bartsch JW, Palmisano R, Zhou P
J. Biol. Chem., 2007;282(49):35712-21. -
A Staphylococcus aureus pore-forming toxin subverts the activity of ADAM10 to cause lethal infection in mice.
Inoshima et al.
Nat.Med., 2011;17:1310 -
Metalloprotease inhibitors for the disintegrin-like metalloproteinases ADAM10 and ADAM17 that differentially block constitutive and phorbol ester-inducible shedding of cell surface molecules.
Ludwig et al.
Comb.Chem.High Throughput Screen., 2005;8:161 -
The disintegrin-like metalloproteinase ADAM10 is involved in constitutive cleavage of CX3CL1 (fractalkine) and regulates CX3CL1-mediates cell-cell adhesion.
Hundhausen et al.
Blood, 2003;102:1186
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Citations for GI 254023X
The citations listed below are publications that use Tocris products. Selected citations for GI 254023X include:
13 Citations: Showing 1 - 10
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Ex vivo analysis platforms for monitoring amyloid precursor protein cleavage.
Authors: Takashi Et al.
Front Mol Neurosci 2023;15:1068990
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Platelets upregulate tumor cell programmed death ligand 1 in an epidermal growth factor receptor-dependent manner in vitro.
Authors: Sandra S Et al.
Blood Adv 2022;6:5668-5675
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Roles for ADAM17 in TNF-R1 Mediated Cell Death and Survival in Human U937 and Jurkat Cells.
Authors: Wulf Et al.
Cells 2021;10
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Shear stress activates ADAM10 sheddase to regulate Notch1 via the Piezo1 force sensor in endothelial cells.
Authors: T Simon Et al.
Elife 2020;9
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Localized Intercellular Transfer of Ephrin-As by Trans-endocytosis Enables Long-Term Signaling.
Authors: Franck Et al.
Dev Cell 2020;52:104-117.e5
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ADAM17-dependent signaling is required for oncogenic human papillomavirus entry platform assembly.
Authors: Mikuličić Et al.
Elife 2019;8
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Vaccinia virus hijacks EGFR signalling to enhance virus spread through rapid and directed infected cell motility.
Authors: Beerli Et al.
Nat Microbiol 2019;4:216
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Visualization of Alzheimer's Disease Related α-/β-/γ-Secretase Ternary Complex by Bimolecular Fluorescence Complementation Based Fluorescence Resonance Energy Transfer.
Authors: Wang and Pei
Front Mol Neurosci 2018;11:431
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Ectodomain shedding of Limbic System-Associated Membrane Protein (LSAMP) by ADAM Metallopeptidases promotes neurite outgrowth in DRG neurons.
Authors: Sanz
Sci Rep 2017;7(1):7961
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ADAM10 Cell Surface Expression but Not Activity Is Critical for Staphylococcus aureus α-Hemolysin-Mediated Activation of the NLRP3 Inflammasome in Human Monocytes.
Authors: Ezekwe Et al.
J Bone Miner Res 2016;8
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Fractalkine shedding is mediated by p38 and the ADAM10 protease under pro-inflammatory conditions inhuman astrocytes.
Authors: O'Sullivan Et al.
Journal of Neuroinflammation 2016;13:189
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Annexin A1-containing extracellular vesicles and polymeric nanoparticles promote epithelial wound repair.
Authors: Leoni Et al.
J Clin Invest 2015;125:1215
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Elevated serum CXCL16 is an independent predictor of poor survival in ovarian cancer and may reflect pro-metastatic ADAM protease activity.
Authors: Gooden Et al.
Br J Cancer 2014;110:1535
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