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Submit ReviewGI 254023X
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)
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 Data for GI 254023X
| 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 391.5. 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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Product Datasheets for GI 254023X
References for GI 254023X
References are publications that support the biological activity of the product.
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
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
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 reference for GI 254023X, please let us know.
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Keywords: GI 254023X, GI 254023X supplier, GI254023X, ADAM10, metalloproteases, MMPs, metalloproteinases, inhibits, inhibitors, adams, Matrix, Metalloprotease, ADAMs, 3995, Tocris Bioscience
13 Citations for GI 254023X
Citations are publications that use Tocris products. Selected citations for GI 254023X include:
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
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
Sandra S et al (2022) Platelets upregulate tumor cell programmed death ligand 1 in an epidermal growth factor receptor-dependent manner in vitro. Blood Adv 6 5668-5675 PMID: 35482455
Takashi et al (2023) Ex vivo analysis platforms for monitoring amyloid precursor protein cleavage. Front Mol Neurosci 15 1068990 PMID: 36683852
Franck et al (2020) Localized Intercellular Transfer of Ephrin-As by Trans-endocytosis Enables Long-Term Signaling. Dev Cell 52 104-117.e5 PMID: 31866204
T Simon et al (2020) Shear stress activates ADAM10 sheddase to regulate Notch1 via the Piezo1 force sensor in endothelial cells. Elife 9 PMID: 32484440
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
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
Sanz (2017) Ectodomain shedding of Limbic System-Associated Membrane Protein (LSAMP) by ADAM Metallopeptidases promotes neurite outgrowth in DRG neurons. Sci Rep 7 7961 PMID: 28801670
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
Wulf et al (2021) Roles for ADAM17 in TNF-R1 Mediated Cell Death and Survival in Human U937 and Jurkat Cells. Cells 10 PMID: 34831323
Leoni et al (2015) Annexin A1-containing extracellular vesicles and polymeric nanoparticles promote epithelial wound repair. J Clin Invest 125 1215 PMID: 25664854
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