229103

Choline Kinase-a Inhibitor, CK37

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.

• Synonyme(s) : Choline Kinase-a Inhibitor, CK37, 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
• Formule empirique (notation de Hill): C₂₀H₂₂N₄OS
• Numéro CAS: 1001478-90-5
• Poids moléculaire : 366.48
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: powder
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: tan
• Solubilité: DMSO: 50 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C
• Chaîne SMILES: O=C(NC1=CC(C)=CC(C)=C1)CSC2=NNC(C3=CC=C(CC)C=C3)=N2

Description

Description générale

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.

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.

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°c.

Autres remarques

Clem, B., et al. 2011. Oncogene30, 3370.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable