WM-1119
| Target | KAT6A KAT6B |
| Targeted domain | AcCoA binding site |
| Mode of action | Inhibitor |
| Control | WM-2474 |
| Recommended cellular usage concentration | 1 µM (≤ 10 µM) |
| In vivo use | yes |
| Synonyms | WM 1119 |
| Donated by | Monash University, SGC Toronto |
Probe criteria
| Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) | Surpasses criterion: KAT6A: Kd = 2 nM (surface plasmon resonance (SPR)); IC50 = 37 nM (HAT activity assay (AlphaScreen)) |
| Selectivity within target family: > 30-fold | > 200-fold selective on all other HATs tested. |
| Selectivity outside target family | No significant activity on 166 targets at 10 μM. (Kinases, GPCRs, HDACs, phosphatases etc.)Closest hits in the PDSP scan are DRD2 (Ki = 397.52 nM) and GABAA/BZP (75.65 % inhibition). |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion: Cell cycle arrest in Fucci MEFs (Mouse Embryonic Fibroblast) at 1 µM. EMRK1184 cell growth inhibited with IC50 = 0.25 µM |
| Control compound (100 times less potent than the probe) | WM-2474: KAT6A IC50 > 50 µM (HAT activity assay (AlphaScreen)); No effect on Fucci MEFs at 10 µM.Clean PDSP scan. |