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Choline Kinase-a Inhibitor, CK37
A cell-permeable, non-Hemicholinium-3 derivative and choline-competitive choline kinase-α inhibitor. It is demonstrated to inhibit endogenous choline kinase activity, dose-dependently, between 1-10 µM, and dose-dependently decrease phosphocholine concentrations, as well as levels of downstream choline metabolites, including phosphatidylcholine and phosphatidic acid in HeLa cells. At 10 µM, it is also shown to attenuate MAPK and PI3K/AKT signaling, and disrupt the actin cytoskeleton and membrane ruffling, consistent with siRNA choline kinase-&alpha transfection. This compound exhibits dose-dependent suppression of cell growth in six tumor cell lines (IC50 = 5-10 µM), in vitro. Furthermore, it is shown to suppress tumor growth in a mouse model by 48% at 0.08 mg/g daily dose for 8 days without obvious toxicity, in vivo.
产品信息
Form Tan powder
Molar mass 366.48
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥97% by HPLC
Solubility DMSO
Chemical formula C20H22N4OS
CAS number 1001478-90-5
商店和运输信息
Storage +2°C to +8°C
Ship Ambient Temperature Only
Standard Handling |