Cat. #151832
LIMK inhibitor CRT0105950 Small Molecule (Tool Compound)
Cat. #: 151832
Sub-type: Inhibitor
Availability: Please enquire for quantities and pricing
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.
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Contributor
Inventor: Mark Charles
Institute: Cancer Research Technology
Tool Details
*FOR RESEARCH USE ONLY
- Tool name: LIMK inhibitor CRT0105950 Small Molecule (Tool Compound)
- Molecular formula: C20H18F3N3O2S
- Tool sub type: Inhibitor
- Primary target: LIMK1 and LIMK2
- 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...
- 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
- Molecular weight: 383.89
- Additional notes: % invasion inhibition at 3uM 52 % cell viability at 10uM 100
Handling
- Purity: 383.89 g/mol
- Shipping conditions: Dry Ice
Target Details
- Primary target: LIMK1 and LIMK2
- Ic50: IC50 LIMK1 0.008uMIC50 LIMK2 0.048uMIC50 Cell p-cofilin 1uM
Application Details
- 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.
References
- Charles et al. 2015. J Med Chem. :. PMID: 26356364
