FS-694
| Target | MAPK14 |
| Targeted domain | Kinase domain (active site) |
| Mode of action | Inhibitor (type 1.5, ATP competitive) |
| Control | FM-743 |
| Orthogonal probe | Skepinone-L SR-318 |
| Recommended cellular usage concentration | 0.1 - 1 µM |
| In vivo use | No |
| Donated by | Uni Tübingen/ SGC FFM |
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd>/sub>) | Surpasses criterion: MAPK14: IC50 = 0.2 nM (ELISA, cell free); KD = 1.5 nM (DiscoverX) |
| Selectivity within target family: > 30-fold | Surpasses criterion: Off targets detected in DX screen inactive in cells (NanoBRET) |
| Selectivity outside target family | N/A |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion:NanaoBRET: MAPK14 IC50 = 14.9 nM; MAPK11 IC50 = 16.9 nM (full-length protein in HEK cells); Western: Inhibition of HSP27 (Ser82) < 1μM |
| On target cell activity for secreted targets: appropriate alternative such as mouse model or other mechanistic biological assay, e.g., explant culture | Inhibition of TNFα release in WB: IC50 = 38 ± 1 nM |
| Control compound (100 times less potent than the probe) | Surpasses criterion: FM-743: IC50 MAPK14/MAPK11 = 11.3/ 16.2 µM (NanoBRET) |