GI 254023X
Tocris Bioscience, part of Bio-Techne | Catalog # 3995
Selective ADAM10 metalloprotease inhibitor
Key Product Details
Description
Selective ADAM10 metalloprotease inhibitor
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
Molecular Weight
391.50
Formula
C21H33N3O4
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
(2R)-N-[(1S)-2,2-Dimethyl-1-[(methylamino)carbonyl]propyl]-2-[(1S)-1-(N-hydroxyformamido)ethyl]-5-phenylpentanamide
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 7.83 | 20 |
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.
| 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
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
- 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 Specific Notices for GI 254023X
For research use only
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