658084-64-1

Usage

Uses

Used in Pharmaceutical Industry:
(E)-N-[4-(1-BENZOYL-PIPERIDIN-4-YL)-BUTYL]-3-PYRIDIN-3-YL-ACRYLAMIDE is used as a research compound for studying its effects on biological systems and potential therapeutic applications. Its unique structure allows it to interact with specific targets, making it a candidate for the development of new drugs and therapies.
Used in Chemical Research:
In the field of chemical research, (E)-N-[4-(1-BENZOYL-PIPERIDIN-4-YL)-BUTYL]-3-PYRIDIN-3-YL-ACRYLAMIDE serves as a valuable tool for understanding the properties and behavior of complex organic molecules. Its synthesis and modification can provide insights into the development of new chemical compounds and materials.
Used in Biochemical Studies:
(E)-N-[4-(1-BENZOYL-PIPERIDIN-4-YL)-BUTYL]-3-PYRIDIN-3-YL-ACRYLAMIDE is used in biochemical studies to investigate its interactions with enzymes, proteins, and other biomolecules. This can help researchers understand its potential role in biological processes and identify new avenues for its application in medicine and other fields.

In vitro

APO866 at low concentrations ranging from 0.09-27 nM induces dose-dependent cytotoxicity in 41 hematologic malignant cells including acute myeloid leukemia [AML], acute lymphoblastic leukemia [ALL], mantle cell lymphoma [MCL], chronic lymphocytic leukemia [CLL], and T-cell lymphoma. APO866 at low concentrations ranging from 0-10 nM induces cell death, this effect is independent of caspase activation but is associated with depolarization of mitochondrial membrane. APO866 at concentrations ranging from 0-10 nM dose-dependently induces depletion of intracellular NAD and ATP contents and cell death in various hematologic cancer cells. APO866 at concentration of 10 nM inhibits PBEF-induced secretion of MMP-3, CCL2, and CXCL8 in HFFF2 cells.

In vivo

APO866 administered intraperitoneally at dose of 20 mg/kg twice a day for 4 days, repeat weekly over 3 weeks, prevents and abrogats tumor growth in C.B.-17 SCID mice xenograft models of human AML, lymphoblastic lymphoma, and leukemia. APO866 at dose of 0.12 mg/kg/hour prevents joint destruction and leukocyte infiltration through inhibition of PBEF in mice with CIA.

Biochem/physiol Actions

FK866 is a potent inhibitor of NAD biosynthesis, and a specific inhibitor of NAMPT (Nicotinamide Phosphoribosyltransferase, visfatin, PBEF). NAMPT functions as an intra-cellular and extra-cellular NAD biosynthetic enzyme that is important for regulating metabolism and stress resistance through sirtuins and other NAD-consuming regulators. NAMPT also acts as a cytokine independent of its enzymatic activity, playing a major part in regulating immune responses.

references

[1] nahimana a, attinger a, aubry d, greaney p, ireson c, thougaard av, tj?rnelund j, dawson km, dupuis m, duchosal ma. the nad biosynthesis inhibitor apo866 has potent antitumor activity against hematologic malignancies. blood. 2009 apr 2; 113 (14): 3276-86.