1425049-46-2

Upstream product

• 111-64-8 n-octanoic acid chloride 
• 103-45-7 acetic acid phenethyl ester 
• 123-75-1 pyrrolidine 
• 162358-06-7 4-octylphenethyl methanesulfonate 
• 162358-03-4 2-(4-octanoylphenyl)ethyl acetate 
• 162358-04-5 acetic acid 2-(4-octylphenyl)ethyl ester 
• 162358-05-6 2-(4-Octylphenyl)ethyl alcohol 

Relevant academic research and scientific papers

SELECTIVE INHIBITORS AND ALLOSTERIC ACTIVATORS OF SPHINGOSINE KINASE

Sphingosine 1-phosphate (S1P) is involved in hyper-proliferative diseases, such as cancer and vascular remodeling in pulmonary arterial hypertension. Inhibitors of sphingosine kinase 1 and 2 (SK1 and SK2), which catalyze the synthesis of S1P, may be useful anti- proliferative agents. We have synthesized a series of sphingosine-based inhibitors of SK and SK2. Also provided in this invention are compounds that activate SK1 which can be used in diseases such as fibrosis, where intracellular S1P is anti-fibrotic.

Synthesis of selective inhibitors of sphingosine kinase 1

Sphingosine kinase isoform 1 (SK1) inhibitors may serve as therapeutic agents for proliferative diseases, including hypertension. We synthesized a series of sphingosine-based SK1-selective inhibitors, the most potent of which is RB-005 (IC50 = 3.6 μM), which also induced proteasomal degradation of SK1 in human pulmonary arterial smooth muscle cells.