LIMK inhibitor CRT0105950 Small Molecule (Tool Compound)

The LIMK inhibitor CRT0105950 is a novel, selective, potent LIMK inhibitor, which inhibits p-cofilin and inhibits invasion in a Matrigel inverse invasion assay.

Contributors

Inventor Institute
Mark Charles Cancer Research Technology
Cat. #: 151832
Tool sub type: Inhibitor
Research Fields: Cell signaling and signal transduction;Metabolism;Neurobiology
Application: The compounds exhibit low uM potency in breast cancer cells showing dose dependent inhibition of phosphorylation of the LIMK substrate cofilin. Treatment of MDA-MB-231 breast cancer cells with the compounds significantly reduces their ability to invade a matrigel plug in an inverse in vitro invasion assay. Furthermore, the inhibitors effectively reduce fibroblast-led collective invasion in a co-culture organotypic model.
Purpose: Inhibitor
Product description: The LIMK inhibitor CRT0105950 is a novel, selective, potent LIMK inhibitor, which inhibits p-cofilin and inhibits invasion in a Matrigel inverse invasion assay. LIMK1 has been reported to play a key role in tumour cell invasion, and the level of LIMK1 is increased in breast and prostate cancer cell lines in comparison with less invasive cell lines. The LIM kinases (LIMK1 and LIMK2) phosphorylate and inactivate cofilin which allows them to act as regulators of actin cytoskeletal dynamics and microtubule organisation.
Additional notes: % invasion inhibition at 3uM 52 % cell viability at 10uM 100
Molecular weight: 383.89
Primary target: LIMK1 and LIMK2
Shipping conditions: Dry Ice
References:

Charles et al. 2015. J Med Chem. :. PMID: 26356364

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