Table 1 IC50 values obtained for each β-subunit

From: Proteasome inhibitor-adapted myeloma cells are largely independent from proteasome activity and show complex proteomic changes, in particular in redox and energy metabolism

 

Proteasome subunit

AMO-1

AMO-BTZ

AMO-CFZ

BTZ

 IC50 (nm) (50% functional proteasome inhibition)

β2c

NA

NA

NA

 

β2i

NA

NA

NA

 

β1c

40

60

50–60

 

β1i

20–25

50

50–60

 

β5c

25

80–90

50–60

 

β5i

30

80–90

50–60

 LD50 (nm) (50% cell viability)

 

50

>1000

>1000

CFZ

 IC50 (nm) (50% functional proteasome inhibition)

β2c

300

220

>1000

 

β2i

180

90

800

 

β1c

>500

600

>1000

 

β1i

>250

250

1000

 

β5c

10

50

90

 

β5i

10

50

250

 LD50 (nm) (50% cell viability)

 

150

>1000

>1000

  1. IC50 values for the inhibition of proteasome β-subunits in AMO-1-sensitive cells and AMO cells adapted to bortezomib (AMO-BTZ) and carfilzomib (AMO-CFZ) during treatment with bortezomib (Btz) and carfilzomib (Cfz), as deferred from subunit-selective activity-based fluorescent labeling, in relation to the LD50 (50% cell viability, determined by MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium)). NA, not applicable or >1000 nm indicate no significant effect on the IC50 value up to 1000 nm.