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.

• Sinónimos: 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
• Fórmula empírica (notación de Hill): C₂₀H₂₂N₄OS
• Número de CAS: 1001478-90-5
• Peso molecular: 366.48
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Ensayo: ≥95% (HPLC)
• Formulario: powder
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: tan
• solubilidad: DMSO: 50 mg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: 2-8°C
• cadena SMILES: O=C(NC1=CC(C)=CC(C)=C1)CSC2=NNC(C3=CC=C(CC)C=C3)=N2
• InChI: 1S/C20H22N4OS/c1-4-15-5-7-16(8-6-15)19-22-20(24-23-19)26-12-18(25)21-17-10-13(2)9-14(3)11-17/h5-11H,4,12H2,1-3H3,(H,21,25)(H,22,23,24)
• Clave InChI: PSJVIOBOAOSNIY-UHFFFAOYSA-N

Descripción

Descripción general

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.

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

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

Otras notas

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

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable