TH-257

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].

Product Specifications

CAS Number

[2244678-29-1]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

LIM Kinase (LIMK)

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage

Applications

Neuroscience-Neuromodulation

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/th-257.html

Purity

98.36

Solubility

DMSO : 250 mg/mL (ultrasonic)

Smiles

O=C(N(CCCC)CC1=CC=CC=C1)C2=CC=C(S(=O)(NC3=CC=CC=C3)=O)C=C2

Molecular Formula

C24H26N2O3S

Molecular Weight

422.54

Precautions

H302, H315, H319, H335

References & Citations

[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.