SM311

2D structure
Target LIMK1 
Targeted domain Active site (covalent binding to Cys349)
Mode of action Covalent inhibitor
Control SM311-NC
Recommended cellular usage concentration 0.1 -1 µM
In vivo use No
Donated by Goethe University Frankfurt


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) Surpasses criterion: TR-FRET assay: KI = 40.71 nM; Kinact = 0.00283 s-1, Kinact/ KI = 69516 M-1s-1
Selectivity within target family: > 30-fold LIMK2: NanoBRET (EC50 = 6.74 µM)
DSF panel: 3 targets > 3 K: LIMK1 (deltaTm = 8.11 K), MAPK8 (deltaTm =7.36 K) , MAPK10 (deltaTm =8.12 K).
NanoBRET K192 (tracer displacement assay at 1 µM): 6 targets > 50 %, LIMK1 (91 %), CDKL2 (85 %), NLK and TXK (73 %), AAK1 (66 %),MAPK9 (JNK2) (65 %)
NanoBRET TE (EC50 [µM]): CDKL2 (1.5), AAK1 (10.4), MAPK8 (23), MAPK9 (14.3), MAPK10 (25.5), STK32B (31), SRC (> 50)
Selectivity outside target family Selectivity for LIMK1 confirmed by whole-cell proteomics
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Surpasses criterion: LIMK1 NanoBRET TE: EC50 = 45 nM
Control compound (100 times less potent than the probe) SM311-NC: LIMK1 NanoBRET TE : EC50 > 25 µM