Cas No.: | 658084-64-1 |
Chemical Name: | (E)-N-(4-(1-benzoylpiperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide |
Synonyms: | APO866; APO-866; APO 866; FK 866; FK-866; FK866; K 22.175; Daporinad; |
SMILES: | O=C(C1=CC=CC=C1)N(CC2)CCC2CCCCNC(/C=C/C3=CC=CN=C3)=O |
Formula: | C24H29N3O2 |
M.Wt: | 391.51 |
Sotrage: | 2 years -20°C powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | FK866 is an effective inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase) with an IC50 of 0.09 nM. |
In Vivo: | 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[1]. |
In Vitro: | Nampt inhibition with FK866 induces significant NAD+ intracellular reduction and selectively kills MM cells. 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 FK866 sensitivity. FK866 abrogates the survival advantage conferred by the bone marrow microenvironment[1]. FK866 prevents the [Ca2+]i increase induced by different mitogens and reduces the Ca2+ content of TG-responsive Ca2+ stores in Jurkat and in activated PBLs. FK866 reduces the Ca2+ content of TG-responsive Ca2+ stores in Jurkat cells but not in Bcl2-Jurkat cells[2]. Inhibition of NAMPT by FK866, or inhibition of SIRT by nicotinamide decreases proliferation and triggered death of 293T cells involving the p53 acetylation pathway[3]. |