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抑制剂/激活剂

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凋亡与自噬

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FK866 (APO866) APO866

Daporinad (FK866)有效抑制烟酰胺磷酸核糖转移酶(NMPRTase; Nampt)，Daporinad (FK866) 可引发自噬，无细胞试验中IC50为0.09 nM。Phase 1/2。

货号：
TK0526
规格：

1mg

5mg

10mg

50mg
价格：
￥0.00

产品参数

CAS No.	658084-64-1
生物活性	(E)-Daporinad (FK866) is an effective inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with an IC50 of 0.09 nM.
分子式	C24H29N3O2
分子量	391.51
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder, -20°C ,3 years
溶解性数据	DMSO : ≥ 50 mg/mL (127.71 mM)，H2O : < 0.1 mg/mL (insoluble)
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.
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.
纯度及产品资料	98%

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