THNAN69
| Target | LIMK2 |
| Targeted domain | ATP binding pocket |
| Mode of action | Degrader |
| Control | THNAN69-NC |
| Recommended cellular usage concentration | 10 - 100 nM |
| In vivo use | No |
| Donated by | Goethe University Frankfurt |
Probe criteria
| Selectivity within target family: > 30-fold | LIMK1: NanoBRET (EC50 = 412 nM), DSF (deltaTM = 6.9 °C), SPR (KD = 249 nM) |
| Selectivity outside target family | Selectivity for LIMK2 confirmed by whole-cell proteomics |
| On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 | Surpasses criterion: LIMK2 NanoBRET: EC50 = 80 nM; EGFP-LIMK2 depletion assay: DC50 = 1 nM; LIMK2 degradation at 10 nM: Dmax = ~90% |
| Control compound (100 times less potent than the probe) | THNAN69-NC: No LIMK2 degradation: Tested at 1 µM in western blot and at up to 10µM in EGFP-LIMK2 assay. DCmax at 10nM = 0% (vs DMSO) The control has a modification that negates proximity completely which is required for PROTACS to work. |