Sphingosine Kinase Inhibitor IV, CB5468139

A cell-permeable naphthoquinone derivative that acts as an ATP-competitive inhibitior against sphingosine kinase 1 (K_i = 280 nM; IC₅₀ = 2 µM; [sphingosine] = 10 µM & [ATP] = 100 µM) and several protein kinases, including, but not limited to, TNK2, AURKB, Met, Syk, AURKC, Fyn, Flt2, PIM2, MST2, CLK1, Tie1, and Fak (% inhibition by 2 µM CB5468139 = 82, 72, 65, 62, 58, 57, 56, 56, 53, 52, 51, and 51, respectively), while exhibiting much reduced potency against DAG Kinase (37% inhibition at 100 µM) and sphingosine kinase 2 (no inhibition at 100 µM; [sphingosine] = 5 µM & [ATP] = 100 µM). CB5468139 is shown to be more potent than SK1/2 dual inhibitor (Cat. No. 567731) against kidney adenocarcinoma A498 proliferation (GI₅₀ = 10 and 20 µM, respectively; 48 h) and the two inhibitors are also reported to induce differential modulations of A498 cellular ceramides and S1P levels when applied at their respective GI₅₀.

Packaged under inert gas

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

Gao, P., et al. 2012. PLoS One.7, e44543.

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

Toxicity: Standard Handling (A)