Table 1.

IC50 values of serine proteases in purified enzymes and PBMC lysates

IC50 (μmol/L)
CarfilzomibBortezomib
TargetP1 selectivityPurified enzymePBMC lysateaPurified enzymePBMC lysatea
CatAF, Y, V, E>10>102.5 (1.6–4.1)0.0047 (0.0022–0.0098)
CatGL, F, H, Y, N, I, V>10>100.95 (0.77–1.2)0.3 (0.12–0.76)
ChymaseF, Y>10>100.28 (0.26–0.31)0.0016 (0.00071–0.0036)
DPPIIP, A, R>10>108.7 (5.6–14)0.26 (0.17–0.4)
HtrA2/OmiL, V>10N/A0.003 (0.001–0.009)N/A
Proteasome (LMP7)L, F0.025 (0.015–0.041)0.022 (0.016–0.030)0.031 (0.021–0.047)0.00099 (0.00063–0.0016)

NOTE: 95% CIs are shown within parenthesis.

Abbreviation: N/A, not available.

aLysate IC50 values were generated by using the ABP method except LMP7 activity which was measured by using a fluorogenic substrate assay.