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TH-257

$73$630

Products Details

Product Description

– 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].

Web ID

– HY-122630

Storage Temperature

– -20°C, 3 years; 4°C, 2 years (Powder)

Shipping

– Room Temperature

Applications

– Neuroscience-Neuromodulation

Molecular Formula

– C24H26N2O3S

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.|[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.

CAS Number

– 2244678-29-1

Molecular Weight

– 422.54

Compound Purity

– 98.01

SMILES

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

Clinical Information

– No Development Reported

Research Area

– Cancer

Solubility

– DMSO : 250 mg/mL (ultrasonic)

Target

– LIM Kinase (LIMK)

Isoform

– LIMK1;LIMK2

Pathway

– Cell Cycle/DNA Damage

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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