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Beschreibung

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 microM in A549 and MDA-MB-231 cultures) without affecting tubulin polymerization or inducing cytotoxicity (EC50 >10 microM in A549 proliferation and colony formation assays). Shown to effectively destabilize F-actin structure in MDA-MB-231 breast cancer cells (3 to 10 microM) with concomitant blockage of invadopedia-mediated ECM degradation (13% and 10% of control, respectively, by 3 and 10 microM inhibitor) and invasion (45% and 7% of control invasion rate, respectively, by 3 and 10 microM inhibitor). Although reported to exhibit affinity toward AMPK&alpha,1 and AMPK&alpha,2 in T7 phage-based competition binding studies, inhibitory activity of LIMKi 3 against AMPK&alpha,1/2 is not yet directly demonstrated., 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 µ,M in A549 and MDA-MB-231 cultures) without affecting tubulin polymerization or inducing cytotoxicity (EC50 >,10 µ,M in A549 proliferation & colony formation assays). Shown to effectively destabilize F-actin structure in MDA-MB-231 breast cancer cells (3 to 10 µ,M) with concomitant blockage of invasion (by 93% at 10 µ,M).