5.09106

Sphingosine Kinase-2 Inhibitor, K145

• Synonyme(s) : Sphingosine Kinase-2 Inhibitor, K145, SphK2 Inhibitor, K145
• Formule empirique (notation de Hill): C₁₈H₂₄N₂O₃S
• Numéro CAS: 1309444-75-4
• Poids moléculaire : 348.46
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: ≥95% (HPLC)
• Niveau de qualité: 100
• Forme: powder
• Puissance: 4.3 μM IC₅₀
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: off-white
• Solubilité: DMSO: 100 mg/mL; water: 2.5 mg/mL
• Température de stockage: 2-8°C

Description

Description générale

A cell permeable, orally bioavailable thiazolidine-2,4-dione derivative that acts as a selective, sphingosine competitive inhibitor of spingosine Kinase -2 (SphK2; IC₅₀ = 4.3 µM; Ki = 6.4 µM), but does not affect the activities of sphingosine kinase-1, ceremide kinase, and ceramide synthase even at high concentration (~10 micro;M). Shown to inhibit the growth of U937 human leukemic monocyte lymphoma cells by inducing apoptosis and inhibiting the phosphorylation of ERK and Akt. Blocks the growth of U937 cells in nude mice and inhibits the growth of JC tumor cells in BALB/c mice without any apparent toxicity.

A cell permeable, orally bioavailable thiazolidine-2,4-dione derivative that acts as a selective, sphingosine competitive inhibitor of spingosine Kinase -2 (SphK2; IC₅₀ = 4.3 µM; Ki = 6.4 µM), but does not affect the activities of sphingosine kinase-1, ceremide kinase, and ceramide synthase even at high concentration (~10 micro;M). Shown to inhibit the growth of U937 human leukemic monocyte lymphoma cells by inducing apoptosis and inhibiting the phosphorylation of ERK and Akt. Blocks the growth of U937 cells in nude mice and inhibits the growth of JC tumor cells in BALB/c mice without any apparent toxicity.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
Sphk2

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 2 months at -20°C.

Autres remarques

Liu, K., et al. 2013. PLos One8, e56471.

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