For research use only. Not for therapeutic Use.
TH-257 is a potent inhibitor of LIMK1 and LIMK2 with IC50 values of 84 nM and 39 nM for LIMK1 and LIMK2, respectively, and it can be used as a chemical probe for LIMK1 and LIMK2. TH-257 is an allosteric inhibitor targeting a binding pocket induced by an αC and DFG-out conformation. TH257 is exquisitely selective and no significant activity against the wider kinome has been observed in the KINOMEscan assay at 1 μM[1].
TH-257 exhibits good biochemical and cellular potencies. But its extremely rapid in vitro clearance renders it unsuitable as a potential in vivo tool[2].
| Catalog Number | I017876 |
| CAS Number | 2244678-29-1 |
| Synonyms | N-benzyl-N-butyl-4-(phenylsulfamoyl)benzamide |
| Molecular Formula | C24H26N2O3S |
| Purity | ≥95% |
| InChI | InChI=1S/C24H26N2O3S/c1-2-3-18-26(19-20-10-6-4-7-11-20)24(27)21-14-16-23(17-15-21)30(28,29)25-22-12-8-5-9-13-22/h4-17,25H,2-3,18-19H2,1H3 |
| InChIKey | VNCIWNGCMAKKEO-UHFFFAOYSA-N |
| SMILES | CCCCN(CC1=CC=CC=C1)C(=O)C2=CC=C(C=C2)S(=O)(=O)NC3=CC=CC=C3 |
| Reference | [1]. Manetti F. Recent advances in the rational design and development of LIM kinase inhibitors are not enough to enter clinical trials. Eur J Med Chem. 2018 Jul 15;155:445-458. [2]. Collins R, et, al. Comparative Analysis of Small-Molecule LIMK1/2 Inhibitors: Chemical Synthesis, Biochemistry, and Cellular Activity. J Med Chem. 2022 Oct 27;65(20):13705-13713. |
