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.

• Synonim(y): 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
• Wzór empiryczny (zapis Hilla): C₁₅H₁₁ClN₂OS · xHCl
• Numer CAS: 1177741-83-1
• Masa cząsteczkowa: 302.78 (free base basis)
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥98% (HPLC)
• Postać: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; desiccated (hygroscopic); protect from light
• kolor: white
• rozpuszczalność: DMSO: 5 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: 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
• Klucz InChI: ZDRVLAOYDGQLFI-UHFFFAOYSA-N

Opis

Opis ogólny

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.

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
GST-hsk

Product competes with ATP.

Reversible: yes

Target IC₅₀: 0.5 µM for GST-hSK

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Carcinogenic / Teratogenic (D)

Rekonstytucja

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

Inne uwagi

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

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 1