GRADE & PURITYMoligand™?Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools.≥98%(HPLC)
Moligand™, ≥98%(HPLC) Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Storage & shipping
Store at 2-8°C Ships Wet ice Check lot-specific COA for exact specifications.
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Quality documents
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
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Literature proof
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Overview
General description:
A cell-permeable pyrazolylthiazolo-isobutyramide compound that acts as a potent LIM kinase inhibitor (IC50 = 7 and 8 nM against LIMK1 and LIMK2, respectively) and effectively suppresses cellular cofilin phosphorylation (IC50 ~ 1 µM in A549 and MDA-MB-231 cultures) without affecting tubulin polymerization or inducing cytotoxicity (EC50 >10 µM in A549 proliferation and colony formation assays). Shown to effectively destabilize F-actin structure in MDA-MB-231 breast cancer cells (3 to 10 µM) with concomitant blockage of invadopedia-mediated ECM degradation (13% and 10% of control, respectively, by 3 and 10 µM inhibitor) and invasion (45% and 7% of control invasion rate, respectively, by 3 and 10 µM inhibitor). Although reported to exhibit affinity toward AMPKα1 and AMPKα2 in T7 phage-based competition binding studies, inhibitory activity of LIMKi 3 against AMPKα1/2 is not yet directly demonstrated.
Potent LIM kinase inhibitor (IC50values are 7 and 8 nM for LIMK1 and LIMK2 respectively). Inhibits cofilin phosphorylation in MDA-MB-231 breast cancer cells. Reduces MDA-MB-231 tumor cell invasion in a 3D matrigel invasion assay.
Storage
Store at 2-8°C
Shipped In
Wet ice
This product requires cold chain shipping. Ground and other economy services are not available.
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of LIM domain kinase 1;Inhibitor of LIM domain kinase 2
This compound belongs to the class of organic compounds known as phenylpyrazoles. These are compounds containing a phenylpyrazole skeleton, which consists of a pyrazole bound to a phenyl group.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
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