A cell-permeable, tri-substituted pyrazol compound that acts as a potent and specific integrin-linked kinase (ILK) inhibitor (IC50=600nM). Shown to have high in vitro anti-proliferative potency against prostrate and breast cancer cell lines (IC50=1 to 2.5uM) while sparing normal epithelial cells. Its effect on cancer cells have been attributed to induction of autophagy and apoptosis. Suppresses ILK-mediated phosphorylation of Akt at Ser473 site, thereby down-regulating the downstream targets, such as GSK-3b and myosin light chain. Also causes a transcriptional repression of the transcription factor Y-Box binding protein 1 (YB-1). Exhibits minimum toxicity in mouse model.Formula:C30H30F3N5OMolecular Weight:553.6Solubility:DMSO (100mg/ml)Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
