GI 254023X

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Cat.No. 3995 - GI 254023X | C21H33N3O4 | CAS No. 260264-93-5
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)
Datasheet
Citations (8)
Reviews
Literature (4)

Biological Activity

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

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 7.83 20

Preparing Stock Solutions

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.

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

Certificate of Analysis / Product Datasheet
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Keywords: GI 254023X, GI 254023X supplier, GI254023X, ADAM10, metalloproteases, MMPs, metalloproteinases, inhibits, inhibitors, adams, Matrix, Metalloprotease, ADAMs, 3995, Tocris Bioscience

8 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

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


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Literature in this Area

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