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Submit ReviewGW 280264X
Description: Potent ADAM10 and ADAM17 inhibitor
Chemical Name: Phenylmethyl N-[(5S)-5-[[(2R,3S)-3-(formylhydroxyamino)-2-(2-methylpropyl)-1-oxohexyl]amino]-6-oxo-6-(2-thiazolylamino)hexyl]carbamate
Purity: ≥98% (HPLC)
Biological Activity for GW 280264X
GW 280264X is a potent ADAM (A Disintegrin and Metalloproteinase) 17 and ADAM10 inhibitor (IC50 values of 8 nM and 11.5 nM, respectively). It inhibits constitutive and PMA-inducible CX3CL1 shedding and increases adhesive properties in CX3CL1 transfected cells (IC50 = 1 μM in COS-7 and ECV-304 cells). GW 280264X treatment in mice significantly improves functional recovery after spinal cord injury.
Compound Libraries for GW 280264X
GW 280264X is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for GW 280264X
| M. Wt | 575.73 |
| Formula | C28H41N5O6S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 866924-39-2 |
| PubChem ID | 91885425 |
| InChI Key | SKJLITFHSZNZMQ-SGNDLWITSA-N |
| Smiles | CCC[C@H](N(C=O)O)[C@H](C(N[C@H](C(NC1=NC=CS1)=O)CCCCNC(OCC2=CC=CC=C2)=O)=O)CC(C)C |
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 GW 280264X
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 57.57 | 100 |
Preparing Stock Solutions for GW 280264X
The following data is based on the product molecular weight 575.73. 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 |
|---|---|---|---|
| 1 mM | 1.74 mL | 8.68 mL | 17.37 mL |
| 5 mM | 0.35 mL | 1.74 mL | 3.47 mL |
| 10 mM | 0.17 mL | 0.87 mL | 1.74 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.35 mL |
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Product Datasheets for GW 280264X
References for GW 280264X
References are publications that support the biological activity of the product.
Hundhausen et al (2003) The disintegrin-like metalloproteinase ADAM10 is involved in constitutive cleavage of CX3CL1 (fractalkine) and regulates CX3CL1-mediated cell-cell adhesion. Blood 102 1186 PMID: 12714508
Sommer et al (2019) ADAM17-deficiency on microglia but not on macrophages promotes phagocytosis and functional recovery after spinal cord injury Brain Behav.Immun. 80 129 PMID: 30851378
If you know of a relevant reference for GW 280264X, please let us know.
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Keywords: GW 280264X, GW 280264X supplier, ADAM10, ADAM17, metalloproteinases, endopeptidases, inhibitors, inhibits, adhesive, adhesion, CX3CL1, GW280264X, ADAMs, Matrix, Metalloprotease, 7030, Tocris Bioscience
1 Citation for GW 280264X
Citations are publications that use Tocris products. Selected citations for GW 280264X include:
Li et al (2023) ADAM10- and γ-secretase-dependent cleavage of the transmembrane protein PTPRT attenuates neurodegeneration in the mouse model of Alzheimer's disease. FASEB J 37 e22734 PMID: 36583697
Do you know of a great paper that uses GW 280264X from Tocris? Please let us know.
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Alzheimer's Disease Poster
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