114802

AdaAhx₃L₃VS

A potent, covalent, cell-permeable, irreversible inhibitor of chymotrypsin-like (50-100 nM), trypsin-like (1-5 µM), and PGPH (0.5-1 µM) activities of the 20S proteasome.

• Synonyme(s) : AdaAhx₃L₃VS, Adamantane-acetyl-(6-aminohexanoyl)₃-(leucinyl)₃-vinyl-(methyl)-sulfone, Proteasome Inhibitor XVI
• Formule empirique (notation de Hill): C₅₀H₈₈N₆O₈S
• Numéro CAS: 389064-25-9
• Poids moléculaire : 933.33
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥90% (HPLC)
• Forme: powder
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: off-white
• Solubilité: DMSO: 5 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −20°C

Description

Description générale

A cell-permeable, peptide vinyl sulfone that acts as a potent, irreversible inhibitor of proteasome activity. Covalently modifies the catalytically active β-subunits of the proteasome. Shown to inhibit the chymotrypsin-like (10-50 nM), trypsin-like (1-5 µM), and the peptidyl glutamyl peptide hydrolyzing (PGPH) (0.5-1 µM) activities of purified 20S proteasomes from rabbit muscle. Inhibits proteasomal degradation of deglycosylated MHC HLA-A2 heavy chain in US11+ cells (~50 µM).

A potent, covalent, cell-permeable, irreversible inhibitor of chymotrypsin-like (50-100 nM), trypsin-like (1-5 µM), and PGPH (0.5-1 µM) activities of the 20S proteasome.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
chymotrypsin-like activity of the 20S proteasome

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 50-100 nM against chymotrypsin-like activity of the 20S proteasome

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Autres remarques

Kessler, B.M., et al. 2001. Chem. Biol.8, 913.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 1
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable