GI 254023X

Key Product Details

Product Description

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.

Product Specifications for GI 254023X

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for GI 254023X

The following data is based on the product molecular weight 391.50.

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

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 72 publications citing the usage of this 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
• 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
• 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

Product Documents for GI 254023X