559300

Safingol

A cell-permeable and reversible lyso-sphingolipid protein kinase C (PKC) inhibitor that competitively interacts at the regulatory phorbol binding domain of PKC.

• Sinonimo/i: Safingol, L- threo-Dihydrosphingosine
• Formula empirica (notazione di Hill): C₁₈H₃₉NO₂
• Numero CAS: 15639-50-6
• Peso molecolare: 301.51
• Numero MDL: MFCD00792847
• Codice UNSPSC: 12352200

Proprietà

• Livello qualitativo: 100
• Saggio: ≥98% (TLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze
• Colore: white
• Solubilità: ethanol: 10 mg/mL; DMSO: 5 mg/mL; methanol: 5 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: −20°C
• InChI: 1S/C18H39NO2/c1-2-3-4-5-6-7-8-9-10-11-12-13-14-15-18(21)17(19)16-20/h17-18,20-21H,2-16,19H2,1H3; OTKJDMGTUTTYMP-UHFFFAOYSA-N

Descrizione

Descrizione generale

A cell-permeable and reversible lyso-sphingolipid protein kinase C (PKC) inhibitor that competitively interacts at the regulatory phorbol binding domain of PKC. Inhibits enzymatic activity and ³H-phorbol dibutyrate binding of purified rat brain PKC (IC₅₀ = 37.5 µM and 31 µM, respectively). Inhibits human PKC_α, the major overexpressed isoenzyme in MCF-7 DOXR cells (IC₅₀ = 40 µM). Enhances the cytotoxic effect of the chemotherapeutic agent Mitomycin C (MMC; Cat. Nos. 47589 and 475820) in gastric cancer cells by promoting drug-induced apoptosis.

A cell-permeable and reversible lyso-sphingolipid protein kinase C (PKC) inhibitor that competitively interacts at the regulatory phorbol binding domain of PKC. Inhibits enzymatic activity and ³H-phorbol dibutyrate binding of purified rat brain PKC (IC₅₀ = 37.5 µM and 31 µM, respectively). Inhibits human PKC_α, the major overexpressed isoenzyme in MCF-7 DOXR cells (IC₅₀ = 40 µM). Enhances the cytotoxic effect of the chemotherapeutic agent mitomycin C (MMC; Cat. No. 47589) in gastric cancer cells by promoting drug-induced apoptosis.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
Enzymatic activity and 3H-phorbol dibutyrate binding of purified rat brain PKC

Product does not compete with ATP.

Reversible: yes

Target IC₅₀: 37.5 µM and 31 µM, inhibiting enzymatic activity and 3H-phorbol dibutyrate binding of purified rat brain PKC, respectively

Attenzione

Toxicity: Irritant (B)

Ricostituzione

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

Altre note

Kedderis, L.B., et al. 1995. Fundam. Appl. Toxicol.25, 201.
Sachs, C.W., et al. 1995. J. Biol. Chem. 270, 26639.
Schwartz, G.K., et al. 1995. J. Natl. Cancer Inst.87,1394.

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