GI 254023X

Cat. No. 3995

GI 254023X C21H33N3O4 [260264-93-5]

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Chemical Name: (2R)-N-[(1S)-2,2-Dimethyl-1-[(methylamino)carbonyl]propyl]-2-[(1S)-1-(N-hydroxyformamido)ethyl]-5-phenylpentanamide

Biological Activity

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.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline.

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.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Inoshima et al (2011) A Staphylococcus aureus pore-forming toxin subverts the activity of ADAM10 to cause lethal infection in mice. Nat.Med. 17 1310. PMID: 21926978.

Moss et al (2007) The ADAM10 prodomain is a specific inhibitor of ADAM10 proteolytic activity and inhibits cellular shedding events. J.Biol.Chem. 282 35712. PMID: 17895248.

Ludwig et al (2005) 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. 8 161. PMID: 15777180.

Hundhausen et al (2003) The disintegrin-like metalloproteinase ADAM10 is involved in constitutive cleavage of CX3CL1 (fractalkine) and regulates CX3CL1-mediates cell-cell adhesion. Blood 102 1186. PMID: 12714508.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for GI 254023X include:

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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Keywords: GI 254023X, supplier, GI254023X, ADAM10, metalloproteases, MMPs, metalloproteinases, inhibits, inhibitors, adams, Tocris Bioscience, ADAMs Inhibitor products

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