TH251 is a LIMK1 and LIMK2 inhibitor with IC 50 s of 52 nM and 47 nM against LIMK1 and LIMK2 , respectively. TH251 binds to inactive αC-out and DFG-out LIMK1 conformations, inhibits unphosphorylated LIMK1 and LIMK2 enzymatic activity, and exhibits unchanged potency despite PAK-mediated phosphorylation of either kinase. TH251 can be used for the research of cancers, glaucoma, and CNS diseases.
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