General description
A cell permeable, orally bioavailable thiazolidine-2,4-dione derivative that acts as a selective, sphingosine competitive inhibitor of spingosine Kinase -2 (SphK2; IC50 = 4.3 µM; Ki = 6.4 µM), but does not affect the activities of sphingosine kinase-1, ceremide kinase, and ceramide synthase even at high concentration (~10 micro;M). Shown to inhibit the growth of U937 human leukemic monocyte lymphoma cells by inducing apoptosis and inhibiting the phosphorylation of ERK and Akt. Blocks the growth of U937 cells in nude mice and inhibits the growth of JC tumor cells in BALB/c mice without any apparent toxicity.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Sphk2
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 months at -20°C.
Other Notes
Liu, K., et al. 2013. PLos One8, e56471.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| assay | ≥95% (HPLC) |
| Quality Level | 100 |
| form | powder |
| potency | 4.3 μM IC50 |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | off-white |
| solubility | DMSO: 100 mg/mL,water: 2.5 mg/mL |
| storage temp. | 2-8°C |
