Cat. No. 3995
Chemical Name: (2R)-N-[(1S)-2,2-Dimethyl-1-[(methy
Biological ActivitySelective 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 InformationSold for research purposes under agreement from GlaxoSmithKline.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Certificate of Analysis / Safety Data Sheet
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.
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.
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.
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.
If you know of a relevant citation for this product please let us know.
View Related Products by Target
Keywords: GI 254023X, supplier, GI254023X, ADAM10, metalloproteases, MMPs, metalloproteinases, inhibits, inhibitors
Find multiple products by catalog number
New Products in this Area
Non-peptide, competitive angiotensin converting enzyme (ACE) inhibitorAprotinin
Competitive serine protease inhibitorTCID
Selective ubiquitin C-terminal hydrolase-L3 (UCH-L3) inhibitor2-MPPA
Selective glutamate carboxypeptidase II (GCP II) inhibitor; orally bioavailableE 64
Potent and irreversible cysteine protease inhibitorAEBSF
Broad spectrum, irreversible inhibitor of serine proteases
Follow @Tocris on Twitter
Tocris is now actively tweeting. For regular updates on news, events and special offers, follow @Tocris on Twitter.