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.
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Synonym(s):
AdaAhx3L3VS, Adamantane-acetyl-(6-aminohexanoyl)₃-(leucinyl)₃-vinyl-(methyl)-sulfone, Proteasome Inhibitor XVI
Empirical Formula (Hill Notation):
C50H88N6O8S
Recommended Products
Quality Level
Assay
≥90% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
off-white
solubility
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
−20°C
General description
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
chymotrypsin-like activity of the 20S proteasome
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
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Kessler, B.M., et al. 2001. Chem. Biol.8, 913.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 1
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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