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SML0789

Sigma-Aldrich

GI254023X

≥98% (HPLC), powder, ADAM10 metalloproteinase inhibitor

Synonyme(s) :

(2R)-N-[(1S)-2,2-Dimethyl-1-[(methylamino)carbonyl]-propyl]-2-[(1S)-1-[formyl(hydroxy)amino]ethyl]-5-phenylpentanamide, GI4023

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About This Item

Formule empirique (notation de Hill):
C21H33N3O4
Numéro CAS:
260264-93-5
Poids moléculaire :
391.50
Numéro MDL:
MFCD19381832
Code UNSPSC :
12352200
ID de substance PubChem :
329825599
Nomenclature NACRES :
NA.77

product name

GI254023X, ≥98% (HPLC)

Niveau de qualité

100

Pureté

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

DMSO: 15 mg/mL, clear

Température de stockage

2-8°C

Chaîne SMILES 

ON(C=O)[C@@H](C)[C@@H](CCCC1=CC=CC=C1)C(N[C@@H](C(C)(C)C)C(NC)=O)=O

InChI

1S/C21H33N3O4/c1-15(24(28)14-25)17(13-9-12-16-10-7-6-8-11-16)19(26)23-18(20(27)22-5)21(2,3)4/h6-8,10-11,14-15,17-18,28H,9,12-13H2,1-5H3,(H,22,27)(H,23,26)/t15-,17+,18+/m0/s1

Clé InChI

GHVMTHKJUAOZJP-CGTJXYLNSA-N

Application

GI254023X has been used to inhibit ADAM10 (ADAM metallopeptidase domain 10).

Actions biochimiques/physiologiques

GI254023X blocks ADAM10 (ADAM metallopeptidase domain 10) activity and decreases human leukocyte antigen (HLA)-mediated cytotoxicity and cleavage of extracellular E-cadherin in epithelial and endothelial cells.
GI254023X is a potent and selective ADAM10 metalloproteinase inhibitor with 100-fold selectivity for the α-secretase ADAM10 over ADAM17 (TACE). In a study using recombinant TACE and ADAM10 ectodomain, the IC50 for GI254023X was 5.3 nM for ADAM10 vs 541 nM for TACE.
GI254023X is a potent and selective ADAM10 metalloproteinase inhibitor.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Consulter la Bibliothèque de documents

Kazuhiro Aoki et al.
Developmental cell, 43(3), 305-317 (2017-11-08)
The biophysical framework of collective cell migration has been extensively investigated in recent years; however, it remains elusive how chemical inputs from neighboring cells are integrated to coordinate the collective movement. Here, we provide evidence that propagation waves of extracellular
The Mouse-specific Splice Variant mRAGE_v4 Encodes a Membrane-bound RAGE that is Resistant to Shedding and does not Contribute to the Production of Soluble RAGE.
Di Maggio S, et al.
PLoS ONE, 11(9), e0153832-e0153832 (2016)
ADAM10 cell surface expression but not activity is critical for Staphylococcus aureus α-hemolysin-mediated activation of the NLRP3 inflammasome in human monocytes.
Ezekwe E A D, et al.
Toxins, 8(4), 95-95 (2016)
Jun Xiang et al.
Molecular therapy. Nucleic acids, 16, 302-312 (2019-04-09)
β-amyloid (Aβ) plays an essential role in the pathogenesis of Alzheimer's disease (AD). Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) is indispensable for Aβ production, and knockout of BACE1 has no overt phenotypes in mouse. Thus, fine modulation of
Mattia Mori et al.
Scientific reports, 7(1), 2213-2213 (2017-05-21)
Notch signaling is considered a rational target in the therapy of several cancers, particularly those harbouring Notch gain of function mutations, including T-cell acute lymphoblastic leukemia (T-ALL). Although currently available Notch-blocking agents are showing anti-tumor activity in preclinical studies, they
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