| Chemical Properties | Back Directory | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMSO:42.25(Max Conc. mg/mL);100.0(Max Conc. mM)
Ethanol:42.25(Max Conc. mg/mL);100.0(Max Conc. mM) | [form ]
powder | [color ]
white to beige | [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]
O=C(C1=CC=C(C=C1)S(NC2=CC=CC=C2)(=O)=O)N(CC3=CC=CC=C3)CCCC |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
TH-257 is a potenttype 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-257please visit the TH-257 probe summary on the Structural Genomics Consortium (SGC) website.
TH-263 is the negative control for the active probeTH-257. TH-263 is available from Sigma. To learn more about and purchase TH-263click here.
To learn about other SGC chemical probesvisit sigma.com/sgc | [IC 50]
LIMK1: 84 nM (IC50); LIMK2: 39 nM (IC50) | [storage]
Store at +4°C | [References]
[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. DOI:10.1016/j.ejmech.2018.06.016
[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. DOI:10.1021/acs.jmedchem.2c00751 |
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