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(E)-Daporinad

CAS No. : 658084-64-1

MCE 站：(E)-Daporinad

产品活性：(E)-Daporinad (FK866) 是烟酰胺磷酸核糖转移酶 (NMPRTase; Nampt) 的有效抑制剂， IC₅₀ 为 0.09 nM。

研究领域：Metabolic Enzyme/Protease  |  Autophagy

作用靶点：NAMPT  |  Autophagy

In Vitro: 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 [Ca²⁺]i increase induced by different mitogens and reduces the Ca²⁺ content of TG-responsive Ca²⁺ stores in Jurkat and in activated PBLs. (E)-Daporinad (FK866) reduces the Ca²⁺ content of TG-responsive Ca²⁺ 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.

In Vivo: (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.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Metabolism/Protease Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  CHS-828  |  STF-118804  |  Nampt-IN-1  |  CB30865  |  CB 300919  |  GPP78  |  Teglarinad chloride  |  LB-60-OF61  |  NAMPT inhibitor-linker 1  |  NAMPT inhibitor-linker 2

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