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Choline Kinase-a Inhibitor, CK37-CAS 1001478-90-5-Calbiochem
产品编号: | 4084018 |
规格: | The Choline Kinase-α Inhibitor, CK37, also referenced under CAS 1001478-90-5, controls the biological activity of Choline Kinase-α. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. |
CAS NO: | 1001478-90-5 |
包装规格: | 5 MG |
产品类别: | 进口试剂 |
品牌: | Sigma-Aldrich |
优惠价: | 立即咨询 |
产品别名
1001478-90-5
Choline Kinase-a Inhibitor, CK37-CAS 1001478-90-5-Calbiochem
CK37, N-(3,5-dimethyl-dimethylphenyl)-2-[[5-(4-ethylphenyl)-1H-1,2,4-triazol-3-yl]sulfanyl]acetamide
N-(3,5-dimethyl-dimethylphenyl)-2-[[5-(4-ethylphenyl)-1H-1,2,4-triazol-3-yl]sulfanyl]acetamide, CK37
结构式
基本信息
Empirical Formula【经验(实验)分子式】 | C20H22N4OS |
Molecular weight | 366.48 |
General description【一般描述】 | 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. 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-α 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. |
Warning【警告】 | Toxicity: Standard Handling (A) |
Reconstitution【重悬】 | Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°c. |
Other Notes【其他说明】 | Clem, B., et al. 2011. Oncogene30, 3370. |
Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
Quality Level【质量水平】 | 100 |
Assay【测定】 | ≥95% (HPLC) |
form【形式】 | powder |
manufacturer/tradename | Calbiochem® |
storage condition【储存条件】 | OK to freeze protect from light |
color【颜色】 | tan |
solubility【溶解性】 | DMSO: 50 mg/mL |
shipped in【运输】 | ambient |
storage temp.【储存温度】 | 2-8℃ |
SMILES string | O=C(NC1=CC(C)=CC(C)=C1)CSC2=NNC(C3=CC=C(CC)C=C3)=N2 |
packaging【包装】 | 5 mg in Glass bottle Packaged under inert gas |
安全信息
Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
WGK | WGK 3 |