567731

Sphingosine Kinase Inhibitor

The Sphingosine Kinase Inhibitor, also referenced under CAS 1177741-83-1, controls the biological activity of Sphingosine Kinase. This small molecule/inhibitor is primarily used for Cell Signaling applications.

• Synonym(e): Sphingosine Kinase Inhibitor, 2-( p-Hydroxyanilino)-4-( p-chlorophenyl) thiazole, HCl, SK Inhibitor I, 2-(p-Hydroxyanilino)-4-(p-chlorophenyl) thiazole, HCl, SK Inhibitor I
• Empirische Formel (Hill-System): C₁₅H₁₁ClN₂OS · xHCl
• CAS-Nummer: 1177741-83-1
• Molekulargewicht: 302.78 (free base basis)
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; desiccated (hygroscopic); protect from light
• Farbe: white
• Löslichkeit: DMSO: 5 mg/mL
• Versandbedingung: ambient
• Lagertemp.: 2-8°C
• InChI: 1S/C15H11ClN2OS.ClH/c16-11-3-1-10(2-4-11)14-9-20-15(18-14)17-12-5-7-13(19)8-6-12;/h1-9,19H,(H,17,18);1H
• InChIKey: ZDRVLAOYDGQLFI-UHFFFAOYSA-N

Beschreibung

Allgemeine Beschreibung

A cell-permeable disubstituted thiazole compound that displays anti-tumor properties. Acts as a potent, substrate competitive, reversible, and highly specific inhibitor of sphingosine kinase (IC₅₀ = 0.5 µM for GST-hSK). Does not affect the kinase activity of hERK2, hPI3K, or PKCα even at concentrations as high as 60 µM. Induces apoptosis in human cancer cells that express the drug transport proteins Pgp or MRP1 (IC₅₀ = ~ 1-5 µM) through inhibiting sphingosine-1-phosphate production.

A cell-permeable, potent non-ATP-competitive, reversible, and specific inhibitor of sphingosine kinase (IC₅₀ = 500 nM for GST-hSK) that also exhibits anti-tumor properties. Does not affect the kinase activity of hERK2, hPI3 K, or PKC_α at cocentrations as high as 60 µM. Shown to induce apoptosis in human cancer cells that express the drug transport proteins Pgp or MRP1 (IC₅₀ ~1-5 µM) by inhibiting sphingosine-1-phosphate production.

Biochem./physiol. Wirkung

Cell permeable: yes

Primary Target
GST-hsk

Product competes with ATP.

Reversible: yes

Target IC₅₀: 0.5 µM for GST-hSK

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Carcinogenic / Teratogenic (D)

Rekonstituierung

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

Sonstige Hinweise

French, K.J., et al. 2003. Cancer Res.63, 5962.

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 1