Table 2. Results of potency and kinetic assays for different VIM-2 inhibitors.
| Compound Name | VIM-2 Ki, μM(a) (mechanism of inhibition) | IC50(b) or Max Inhibition @ Tested Concentration(c) | ||||
|---|---|---|---|---|---|---|
| VIM-2 (Nitrocefin) | VIM-2 (CCF2) | IMP-1 Nitrocefin | TEM-1 Nitrocefin | AmpC Nitrocefin | ||
| Mitoxantrone | 1.5 + 0.2 (noncompetitive) |
0.63 ± 0.04 μM (67% @ 44 μM) |
ND(d) | >56 (0% @ 56 μM) |
>25 (0% @ 25 μM) |
>25 (0% @ 25 μM) |
| pCMB | (Slowly reversible or irreversible) | NA(e) (80% @ 15 μM) |
NA (83% @ 36 μM) |
NA (82% @ 140 μM) |
>25 (0% @ 25 μM) |
>25 (0% @ 25 μM) |
| 1 | 0.41 ± 0.03 (competitive) |
3.3 ± 0.4 μM (79% @ 56 μM) |
1.3 ± 0.1 μM (76% @ 44 μM) |
>56 (0% @ 56 μM) |
>25 (0% @ 25 μM) |
>25 (0% @ 25 μM) |
| 2 | 1.41 ± 0.12 (competitive) |
7.3 ± 1.9 μM (74% @ 56 μM) |
4.1 ± 0.3 μM (90% @ 44 μM) |
>56 (0% @ 56 μM) |
>25 (0% @ 25 μM) |
>25 (0% @ 25 μM) |
(a)
Ki ± error reported as the standard deviation of 4 replicates.
(b)
IC50 ± error reported as the standard deviation of 3 replicates.
(c)
In parenthesis maximum inhibition achieved at the indicated concentration.
(d)
ND - Not determined due to assay artifact.
(e)
NA – Not applicable due to the nature of inhibition.