Biological Activity
TH-257 is a potent, type III allosteric LIM-kinase (LIMK1 & LIMK2) inhibitor (LIMK1/2 IC50 in nM = 48/29 by cell-free kinase assay and 250/150 by live cell NanoBRET assay using respective transfectants) th at targets LIMK1/2 DFG-out conformation in a non-ATP-competitive manner and exhibits no significant off-target activity by KINOMEscan assay at 1 μM. TH-263 is a structure analog and the recommended negative control for TH-257. For characterization details of TH-257, please visit the
TH-257 probe summary on the Structural Genomics Consortium (SGC) website.
TH-263 is the negative control for the active probe, TH-257. TH-263 is available from Sigma. To learn more about and purchase TH-263,
click here.
To learn about other SGC chemical probes, visit
sigma.com/sgc