TABLE 1.
MLT-943 pharmacology in human cells and cross-species comparison.
| MLT-943 chemical structure | |||
 | |||
| MLT-943 pharmacology testing | Stimulus | IC50 (μM) | Extent of inhibition (%) |
| Human | |||
| IL-2 reporter gene assay (Jurkat T cells) | PMA/CD28 | 0.04 ± 0.02 | >90 |
| IL-2 release (primary T cells) | CD3/CD28 | 0.010 ± 0.002 | >90 |
| CYLD cleavage (primary T cells) | PMA/ionomycin | 0.06 ± 0.007 | >90 |
| IL-2 release (PBMC) | PMA/ionomycin | 0.074 (N = 1) | >80 |
| IL-2 release (50% whole blood) RAT | PMA/CD28 | 0.80 ± 0.20 | >90 |
| Rat | |||
| IL-2 release (50% whole blood) | PMA/CD28 | 0.58 + 0.15 | >90 |
| Dog | |||
| IL-2 release (PBMC) | PMA/ionomycin | 0.092 (N = 1) | >80 |
| IL-2 release (50% whole blood) | PMA/CD28 | 0.58 + 0.04 | >90 |