Adenovirus Proteinase Inhibitor, NSC 37249

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 (K_i = 150 nM) and AVP-pVIc substrate-binding site (K_i = 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 (K_i = 150 nM) and AVP-pVIc substrate-binding site (K_i = 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.

Primary Target
AVP co-factor pVIc (GVQSLKRRRCF) N-terminal binding pocket

Reversible: yes

Secondary Target
AVP-pVIc substrate-binding site

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

McGrath, W.J., et al. 2013. FEBS Lett.587, 2332.

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