Name: GI 254023X
Price: 437.00 USD

- Overview
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    Background
    
    Description:IC50: 5.3 nM (ADAM10)A Disintegrin and metalloproteinase domain-containing protein 10, also known as ADAM10 or CDw156 or CD156c is a protein that in humans is encoded by the ADAM10 gene. ADAM10 (EC#: 3.4.24.81) is a sheddase, and has a broad specificity for peptide hydrolysis reactions (http://en.wikipedia.org/wiki/ADAM10). GI 254023X, synthesized by GSK, was reported to inhibit ADAM10 100-fold over ADAM17. GI 254023X could reduce constitutive cleavage of fractilkine from ECV-304 transfectants [1].In vitro: Previous study reported that compound GI254023X possessed comparable inhibitory potency for ADAM10 only and blocked TACE with more than 100-fold reduced potency [2].In vivo: To examine the ability of GI254023X to inhibit Hla-mediated endothelial barrier disruption in vivo, mice treated for a 3-day period with GI254023X via intraperitoneal injection were subjected to a Miles assay following subcutaneous injection of recombinant toxin. Resutls showed that although all experimental animals succumbed to the lethal challenge, GI254023X-treated mice were less ill in appearance and demonstrated prolongation of time to death [3]. Clinical trial: GI254023X is currently in the preclinical development and no clinical trial is ongoing.
    
    [1] Koichi Yokota, and Shin-Ichiro Nishimura. MMP/ADAM inhibitors: therapeutic potential for psoriasis. Expert Opin. Ther. Patents. 2005;15:421-435
    [2] Hundhausen C, Misztela D, Berkhout TA, Broadway N, Saftig P, Reiss K, Hartmann D, Fahrenholz F, Postina R, Matthews V, Kallen KJ, Rose-John S, Ludwig A.The disintegrin-like metalloproteinase ADAM10 is involved in constitutive cleavage of CX3CL1 (fractalkine) and regulates CX3CL1-mediated cell-cell adhesion. Blood. 2003;102(4):1186-95.
    [3] Powers ME, Kim HK, Wang Y, Bubeck Wardenburg J.ADAM10 mediates vascular injury induced by Staphylococcus aureus α-hemolysin. J Infect Dis. 2012;206(3):352-6.
- Properties
  - Alternative Name
    
    (2R)-N-[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]-2-[(1S)-1-[formyl(hydroxy)amino]ethyl]-5-phenylpentanamide
    
    CAS Number
    
    260264-93-5
    
    Molecular Formula
    
    C21H33N3O4
    
    Molecular Weight
    
    391.5
    
    Appearance
    
    White solid
    
    Purity
    
    98.00%
    
    Solubility
    
    Soluble in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Gao Y, Yang F, et al. "β1,6 GlcNAc branches-modified protein tyrosine phosphatase Mu attenuates its tyrosine phosphatase activity and promotes glioma cell migration through PLCγ-PKC pathways." Biochem Biophys Res Commun. 2018 Oct 28;505(2):569-577. PMID:30274773
    2. Feng L, Wang Y, et al. "ADAM10-Notch signaling governs the recruitment of ovarian pregranulosa cells and controls folliculogenesis in mice." J Cell Sci. 2016 Jun 1;129(11):2202-12. PMID:27084580

GI 254023X

GI 254023X

Background

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