SPHINGOSINE KINASE-2 INHIBITOR K145 (C15-1304-504)

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.

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Molecular Weight: 348.46. Empirical Formula: C₁₈H₂₄N₂O₃S. Assay: ≥. 95% (HPLC). Quality Level: 100. form: powder. potency: 4.3 . μ. M 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. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.