An inhibitor of LIMK2; reduces p-cofilin in Nf1-/- MEFs (IC50 = 30 µM); decreases actin stress fiber formation

T5601640 – 10 mg

Brand:
Cayman
CAS:
924473-59-6
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

T5601640 is an inhibitor of LIM kinase 2 (LIMK2) that inhibits LIMK2-mediated cofilin phosphorylation.{41239} It reduces the levels of phosphorylated cofilin (p-cofilin) in mouse embryonic fibroblasts (MEF) lacking neurofibromin (Nf1-/-; IC50 = 30 µM), which normally have high levels of p-cofilin. T5601640 (50 µM) decreases actin stress fiber formation, inhibits cell migration, and inhibits colony formation of Nf1-/- MEF cells. It inhibits proliferation of ST88-14, U87, and PANC-1 cells with IC50 values of 18.3, 7.4, and 35.2 µM, respectively, and also decreases p-cofilin levels by 20, 24, and 46%, respectively.{41240} Oral gavage administration of T5601640 (60 mg/kg) decreases tumor volume and cofilin phosphorylation in a PANC-1 nude mouse xenograft model.  

 

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Description

An inhibitor of LIMK2; reduces p-cofilin in Nf1-/- MEFs (IC50 = 30 µM); decreases actin stress fiber formation, inhibits cell migration, and inhibits colony formation when used at a concentration of 50 µM; inhibits proliferation of ST88-14, U87, and PANC-1 cells (IC50s = 18.3, 7.4, and 35.2 µM, respectively); decreases p-cofilin levels by 20, 24, and 46% in ST88-14, U87, and PANC-1 cells, respectively; decreases tumor volume in a PANC-1 nude mouse xenograft model when used at a dose of 60 mg/kg

Formal name: 3-methyl-N-[3-[[[3-(trifluoromethyl)phenyl]amino]carbonyl]phenyl]-5-isoxazolecarboxamide

Synonyms:  T56-LIM Kinase Inhibito|T56-LIMKi

Molecular weight: 389.3

CAS: 924473-59-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling||Research Area|Cell Biology|Cytoskeleton & Motor Proteins

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