GW 280264X

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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)
Citations (1)
Literature (1)

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
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
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.

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

Certificate of Analysis / Product Datasheet
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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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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Alzheimer's Disease Poster

Alzheimer's Disease Poster

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