(E)-Daporinad (FK866) is an effective inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with an IC50 of 0.09 nM.
IC50&Target
IC50: 0.09 nM (NMPRTase)
体外研究
Nampt inhibition with (E)-Daporinad (FK866) induces significant NAD intracellular reduction and selectively kills MM cells. (E)-Daporinad (FK866)-induced cell death is associated with inhibition of Nampt activity, rather than protein expression, and higher NAD baseline levels in MM cells than normal PBMCs confer (E)-Daporinad (FK866) sensitivity. (E)-Daporinad (FK866) abrogates the survival advantage conferred by the bone marrow microenvironment. (E)-Daporinad (FK866) prevents the [Ca]i increase induced by different mitogens and reduces the Ca content of TG-responsive Ca stores in Jurkat and in activated PBLs. (E)-Daporinad (FK866) reduces the Ca content of TG-responsive Ca stores in Jurkat cells but not in Bcl2-Jurkat cells. Inhibition of NAMPT by (E)-Daporinad (FK866), or inhibition of SIRT by nicotinamide decreases proliferation and triggered death of 293T cells involving the p53 acetylation pathway.
体内研究
(E)-Daporinad (FK866) (30 mg/kg, i.p.) decreases the tumor burden in CB17-SCID mice, and the tumor tissue demonstrates a significant decrease in ERK phosphorylation and proteolytic cleavage of LC3.
分子式
C24H29N3O2
分子量
391.51
CAS号
658084-64-1
中文名称
达珀利奈
运输条件
Room temperature in continental US; may vary elsewhere.