General description
A sulfonyldiphenylene-bis-dicyclohexylaminoacetamide compound that acts as a potent and selective inhibitor against adenovirus AVP, the cysteine proteinase critical for virion assembly and maturation, by targeting simultaneously AVP co-factor pVIc (GVQSLKRRRCF) N-terminal binding pocket (Ki = 150 nM) and AVP-pVIc substrate-binding site (Ki = 400 nM), blocking not only AVP-pVIc active complex formation/AVP activation (IC50 = 140 nM; [substrate] = 5 µM & [pVIc] = 40 µM), but also AVP-pVIc active complex catalytic activity (IC50 = 490 nM; [substrate] = 5 µM). Does not affect the activity of the serine protease trypsin or the cysteine protease papain even at concentrations as high as 10 µM.
A sulfonyldiphenylene-bis-dicyclohexylaminoacetamide compound that acts as a potent and selective inhibitor against adenovirus cysteine proteinase AVP by targeting simultaneously AVP co-factor pVIc (GVQSLKRRRCF) N-terminal binding pocket (Ki = 150 nM) and AVP-pVIc substrate-binding site (Ki = 400 nM), blocking both AVP-pVIc active complex formation (IC50 = 140 nM; [substrate] = 5 µM & [pVIc] = 40 µM) and catalytic activity (IC50 = 490 nM; [substrate] = 5 µM) without affecting trypsin or papain protease activity even at concentrations as high as 10 µM.
Biochem/physiol Actions
Primary Target
AVP co-factor pVIc (GVQSLKRRRCF) N-terminal binding pocket
Reversible: yes
Secondary Target
AVP-pVIc substrate-binding site
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 6 months at -20°C.
Other Notes
McGrath, W.J., et al. 2013. FEBS Lett.587, 2332.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 41106500
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5058550001