Table 1 IC50 values [μM] of CSN5 inhibitors against JAMM domain proteases and other metalloproteinases.
From: Targeted inhibition of the COP9 signalosome for treatment of cancer
Protease | CSN5i-1b | CSN5i-2 | CSN5i-2e | CSN5i-3 |
|---|---|---|---|---|
CSN5* | 1.1±0.5 (n=14) | 0.002±0.001 (n=2) | 2.1±1.8 (n=2) | 0.0058±0.0005 (n=5) |
AMSHLP* | >100 | >100 | >100 | >100 |
RPN11* | ND | ND | ND | 53±26 (n=2) |
MMP1 | ND | ND | ND | >100 |
MMP2 | >100 | 89±3 (n=2) | ≥90 | >100 |
MMP8 | >100 | 59±8 (n=2) | 48±8 (n=2) | 14.0±0.1 (n=2) |
MMP9 | >100 | 3.8±0.4 (n=2) | 3.2±0.2 (n=2) | 7.4±2.0 (n=2) |
MMP12 | >100 | >100 | >100 | >100 |
MMP13 | >100 | >100 | >100 | >100 |
MMP14 | >100 | 15.40±0.02 (n=2) | 11±1 (n=2) | 4.6±0.5 (n=2) |
ADAM17 | >100 | >100 | >100 | >100 |
