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.

• Synonyme(s) : Safingol, L- threo-Dihydrosphingosine
• Formule empirique (notation de Hill): C₁₈H₃₉NO₂
• Numéro CAS: 15639-50-6
• Poids moléculaire : 301.51
• Numéro MDL: MFCD00792847
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (TLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze
• Couleur: white
• Solubilité: ethanol: 10 mg/mL; DMSO: 5 mg/mL; methanol: 5 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −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
• Clé InChI: OTKJDMGTUTTYMP-UHFFFAOYSA-N

Description

Description générale

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.

Actions biochimiques/physiologiques

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

Avertissement

Toxicity: Irritant (B)

Reconstitution

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

Autres remarques

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.

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