Sphingosine Kinase Inhibitor IV, CB5468139 (N-(3-chloro-1,4-dioxo-1,4-dihydro-2-naphthalenyl)-N-cyclohexylacetamide, SK Inhibitor IV, Sphingosine Kinase Inhibitor IV)

Blue Ice

331, 8

Supplied as a yellow powder.

A cell-permeable naphthoquinone derivative that acts as an ATP-competitive inhibitior against sphingosine kinase 1 (IC50 = 2uM; [sphingosine] = 10uM & [ATP] = 100uM) and several protein kinases, including, but not limited to, TNK2, AURKB, Met, Syk, AURKC, Fyn, Flt2, PIM2, MST2, CLK1, Tie1, and Fak (IC50 <2uM), while exhibiting much reduced potency toward DAG Kinase and sphingosine kinase 2 (37% and no inhibition, respectively, at 100uM). Shown to be more potent than SK1/2 dual inhibitor against kidney adenocarcinoma A498 proliferation (GI50 = 10 and 20uM, respectively; 48h) and the two inhibitors are also reported to induce differential modulations of A498 cellular ceramides and S1P levels when applied at their respective GI50.

Synonyms:
N-(3-chloro-1, 4-dioxo-1, 4-dihydro-2-naphthalenyl)-N-cyclohexylacetamide, SK Inhibitor IV, Sphingosine Kinase Inhibitor IV

Formula:
C₁₈H₁₈ClNO₃

Solubility:
DMSO

Molar Mass:
331.8

Storage and Stability:
Store at 4°C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.