Sphingosine Kinase Inhibitor-CAS 1177741-83-1-Calbiochem

C₁₅H₁₁ClN₂OS · xHCl

302.78 (free base basis)

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.

Cell permeable: yes
Product competes with ATP.
Reversible: yes
Target IC₅₀: 0.5 µM for GST-hSK
Primary Target
GST-hsk

Toxicity: Carcinogenic / Teratogenic (D)

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

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

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

100

≥98% (HPLC)

solid

Calbiochem^®

OK to freeze
desiccated (hygroscopic)
protect from light

white

DMSO: 5 mg/mL

ambient

2-8℃

10 mg in Plastic ampoule
Packaged under inert gas

11 - Combustible Solids

WGK 1