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Biological Activity for TH 257
TH 257 is a potent and selective allosteric LIMK 1/2 inhibitor (IC50 values are 84 and 39 nM, respectively). Inhibits cofilin phosphorylation in vitro. Exhibits no significant activity against the wider kinome.
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the TH 257 probe summary on the SGC website.
Compound Libraries for TH 257
Technical Data for TH 257
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for TH 257
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for TH 257
The following data is based on the product molecular weight 422.54. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.37 mL||11.83 mL||23.67 mL|
|5 mM||0.47 mL||2.37 mL||4.73 mL|
|10 mM||0.24 mL||1.18 mL||2.37 mL|
|50 mM||0.05 mL||0.24 mL||0.47 mL|
References for TH 257
References are publications that support the biological activity of the product.
Manetti et al (2018) Recent advances in the rational design and development of LIM kinase inhibitors are not enough to enter clinical trials. Eur.J.Med.Chem. 155 445 PMID: 29908439
If you know of a relevant reference for TH 257, please let us know.
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Keywords: TH 257, TH 257 supplier, TH257, Potent, selective, LIMK1/2, LIMK1, LIMK2, inhibitors, inhibits, lim, kinases, LIMK, 6899, Tocris Bioscience
Citations for TH 257
Citations are publications that use Tocris products.
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Reviews for TH 257
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Literature in this Area
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Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.