GI 254023X

Name: GI 254023X
Brand: Tocris Bioscience
SKU: 3995

Tocris Bioscience a Bio-Techne Brand

Catalog # 3995

Citations (8)

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Key Product Details

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% (HPLC)
Molecular Weight:	391.5

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Biological Activity for GI 254023X

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.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline.

Technical Data for GI 254023X

M. Wt	391.5
Formula	C₂₁H₃₃N₃O₄
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	260264-93-5
PubChem ID	9952396
InChi Key	GHVMTHKJUAOZJP-CGTJXYLNSA-N
Smiles	CNC([C@H]([C@@](C)(C)C)NC([C@H](CCCC1=CC=CC=C1)[C@H](C)N(O)C([H])=O)=O)=O

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.

Solubility for GI 254023X

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	7.83	20

Preparing Stock Solutions for GI 254023X

The following data is based on the product molecular weight 391.5.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.2 mM	12.77 mL	63.86 mL	127.71 mL
1 mM	2.55 mL	12.77 mL	25.54 mL
2 mM	1.28 mL	6.39 mL	12.77 mL
10 mM	0.26 mL	1.28 mL	2.55 mL

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References for GI 254023X

References are publications that support the biological activity of the product.

Inoshima A Staphylococcus aureus pore-forming toxin subverts the activity of ADAM10 to cause lethal infection in mice. Nat.Med. 2011 PMID: 21926978
Moss The ADAM10 prodomain is a specific inhibitor of ADAM10 proteolytic activity and inhibits cellular shedding events. J.Biol.Chem. 2007 PMID: 17895248
Ludwig Metalloprotease inhibitors for the disintegrin-like metalloproteinases ADAM10 and ADAM17 that differentially block constitutive and phorbol ester-inducible shedding of cell surface molecules. Comb.Chem.High Throughput Screen. 2005 PMID: 15777180
Hundhausen The disintegrin-like metalloproteinase ADAM10 is involved in constitutive cleavage of CX3CL1 (fractalkine) and regulates CX3CL1-mediates cell-cell adhesion. Blood 2003 PMID: 12714508

Citations for GI 254023X (8)

Showing 1 - 8 of 8 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for GI 254023X include:

Mikuličić et al. (2019) ADAM17-dependent signaling is required for oncogenic human papillomavirus entry platform assembly. Elife. 8
PMID: 31107240
Beerli et al. (2019) Vaccinia virus hijacks EGFR signalling to enhance virus spread through rapid and directed infected cell motility. Nat Microbiol. 4:216
PMID: 30420785
Wang and Pei (2018) Visualization of Alzheimer's Disease Related α-/β-/γ-Secretase Ternary Complex by Bimolecular Fluorescence Complementation Based Fluorescence Resonance Energy Transfer. Front Mol Neurosci. 11:431
PMID: 30538620
Sanz (2017) Ectodomain shedding of Limbic System-Associated Membrane Protein (LSAMP) by ADAM Metallopeptidases promotes neurite outgrowth in DRG neurons. Sci Rep. 7(1):7961
PMID: 28801670
Ezekwe et al. (2016) ADAM10 Cell Surface Expression but Not Activity Is Critical for Staphylococcus aureus α-Hemolysin-Mediated Activation of the NLRP3 Inflammasome in Human Monocytes. J Bone Miner Res. 8
PMID: 27043625
O'Sullivan et al. (2016) Fractalkine shedding is mediated by p38 and the ADAM10 protease under pro-inflammatory conditions inhuman astrocytes. Journal of Neuroinflammation. 13:189
PMID: 27549131
Leoni et al. (2015) Annexin A1-containing extracellular vesicles and polymeric nanoparticles promote epithelial wound repair. J Clin Invest. 125:1215
PMID: 25664854
Gooden et al. (2014) Elevated serum CXCL16 is an independent predictor of poor survival in ovarian cancer and may reflect pro-metastatic ADAM protease activity. Br J Cancer. 110:1535
PMID: 24518602

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Showing 1 - 8 of 8 citations Showing All

Product Documents for GI 254023X

COA

Certificate of Analysis

To download a Certificate of Analysis, please select a batch below.