Adenovirus Proteinase Inhibitor; NSC 37249

Biochem/physiol Actions

Secondary TargetAVP-pVIc substrate-binding site

Reversible: yes

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

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 (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.

Legal Information

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

Other Notes

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

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Standard Handling (A)