Table 2.
Number | Jurkat IC50a (μM) | KHYG-1 inhibitionb (% at 20 μM) | KHYG-1 viabilityc (%) | Plasma stabilityd (% at 24 h) |
|
---|---|---|---|---|---|
Mouse | Human | ||||
23 | 0.18 | 63 | 90 | 75 | 46 |
48 | 0.67 | 20 | 92 | 75 | 49 |
59 | 0.90 | 13 | 79 | 87 | 73 |
63 | 1.09 | No activity | — | 80 | 70 |
67 | 0.92 | 80 | 82 | 66 | 39 |
Data given for five most potent compounds as determined by the Jurkat assay.
Inhibition by compound (20 μM) of the perforin-induced lysis of K562 target cells when co-incubated with KHYG-1 human NK cells (see Supplementary data). Percent inhibition calculated compared to untreated control.
Viability of KHYG-1 NK cells after 24 h by Trypan blue exclusion assay (see Supplementary data).
Data given as % parent measured at 24 h in mouse and human plasma (see Supplementary data for further details).