AS1604498

AS1604498 is a highly specific, competitive inhibitor of human NAMPT, with an IC50 of 44.4 nM. It functionally suppresses NAMPT enzyme activity, reducing the production of nicotinamide mononucleotide and decreasing intracellular NAD levels, which activates caspase 3/7 and induces apoptosis in cancer cells. AS1604498 can be utilized in research related to chronic myeloid leukemia.

AS1604498, when administered at concentrations ranging from 0.032 to 10 μM for 48 hours, inhibits the growth of the human leukemia cell line THP-1 with an IC50 of 198 nM, and this effect can be reversed by 10 mM Nicotinamide. In addition, AS1604498 (0.032-10 μM; 48 h) suppresses the growth of the human chronic myelogenous leukemia cell line K562 with an IC50 of 673 nM, and this action is also reversible by 10 mM Nicotinamide. At a concentration of 10 μM for 48 hours, AS1604498 induces delayed activation of caspase 3/7 in THP-1 cells, which can be reversed by 10 mM Nicotinamide. Furthermore, AS1604498, in a dose-dependent manner between 0.001 and 10 μM over 5 hours, reduces NAD levels in K562 cells, with this effect being reversible by 10 mM Nicotinamide.