5.09106

Sphingosine Kinase-2 Inhibitor, K145

• Sinonimo/i: Sphingosine Kinase-2 Inhibitor, K145, SphK2 Inhibitor, K145
• Formula empirica (notazione di Hill): C₁₈H₂₄N₂O₃S
• Numero CAS: 1309444-75-4
• Peso molecolare: 348.46
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Saggio: ≥95% (HPLC)
• Livello qualitativo: 100
• Forma fisica: powder
• Potenza: 4.3 μM IC₅₀
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: off-white
• Solubilità: DMSO: 100 mg/mL; water: 2.5 mg/mL
• Temperatura di conservazione: 2-8°C

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
Sphk2

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 months at -20°C.

Altre note

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

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable