Table 1.

Potency of metalloproteinase inhibitors used in the current study for inhibition of recombinant TACE and ADAM10 ectodomain



IC50, nM*

Selectivity
Compound
TACE
ADAM10
ADAM10 potency/TACE potency
GI254023X   541.0   5.3   102.0  
GW280264X
 
8.0
 
11.5
 
1.4
 


IC50, nM*

Selectivity
Compound
TACE
ADAM10
ADAM10 potency/TACE potency
GI254023X   541.0   5.3   102.0  
GW280264X
 
8.0
 
11.5
 
1.4
 
*

The inhibitor concentration leading to half maximal inhibition (IC50) of recombinant TACE or ADAM10 ectodomain was determined as described in “Materials and methods.”

Potency is defined as 1/IC50.

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