85-2072-18　Choline Kinase-a Inhibitor, CK37 (CK37, N-(3,5-dimethyl-dimethylphenyl)-2-[[5-(4-ethylphenyl)-1H-1,2,4-triazol-3-yl]sulfanyl]acetamide) 5mg　CAS No:1001478-90-5　217274

特徴

• A cell-permeable, non-Hemicholinium-3 derivative and choline-competitive choline kinase-a inhibitor. It is demonstrated to inhibit endogenous choline kinase activity, dose-dependently, between 1-10uM, and dose-dependently decrease phosphocholine concentrations, as well as levels of downstream choline metabolites, including phosphatidylcholine and phosphatidic acid in HeLa cells. At 10uM, it is also shown to attenuate MAPK and PI3K/AKT signaling, and disrupt the actin cytoskeleton and membrane ruffling, consistent with siRNA choline kinase-a transfection. This compound exhibits dose-dependent suppression of cell growth in six tumor cell lines (IC50=5-10uM), in vitro. Furthermore, it is shown to suppress tumor growth in a mouse model by 48% at 0.08mg/g daily dose for 8 days without obvious toxicity, in vivo.
• Formula:C20H22N4OS
• Molecular Weight:366.5
• Solubility:DMSO
• 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.