(E)-Daporinad

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Chemical Structure| 658084-64-1 同义名 : APO866; FK866; K 22.175; Daporinad
CAS号 : 658084-64-1
货号 : A129216
分子式 : C24H29N3O2
纯度 : 99%+
分子量 : 391.51
MDL号 : MFCD10565943
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(127.71 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • Transferase

    NMPRTase, Ki:0.4 nM
描述 Nampt inhibition by (E)-Daporinad (FK866) leads to a significant reduction in NAD+ levels intracellularly, selectively killing multiple myeloma (MM) cells. The cell death induced by (E)-Daporinad is linked to the inhibition of Nampt activity, not its protein expression. MM cells, having higher baseline NAD+ levels compared to normal peripheral blood mononuclear cells (PBMCs), are more susceptible to (E)-Daporinad. Additionally, (E)-Daporinad neutralizes the survival benefits that the bone marrow microenvironment confers on MM cells[1]. (E)-Daporinad (FK866) inhibits the increase in intracellular calcium ([Ca2+].i) that is typically induced by various mitogens and decreases the calcium content of thapsigargin-responsive calcium stores in Jurkat cells and activated peripheral blood lymphocytes (PBLs). However, it does not affect the calcium content in Bcl2-overexpressing Jurkat cells[2]. The inhibition of NAMPT by (E)-Daporinad (FK866), or SIRT by nicotinamide, reduces cell proliferation and induces cell death in 293T cells. This effect involves the p53 acetylation pathway, highlighting a critical regulatory mechanism in cell survival and death[3].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
human A2780 cells Proliferation assay 72 h Antiproliferative activity against human A2780 cells after 72 hrs by sulforhodamine B assay, IC50=1 nM 24405419
human A431 cells Cytotoxic assay Cytotoxicity against human A431 cells by clonogenic assay, IC50=6.1 nM 24164086
human A549 cells Cytotoxic assay 6 days Cytotoxicity against human A549 cells after 6 days by SRB assay, IC50=0.16 μM 21330015
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.55mL

0.51mL

0.26mL

12.77mL

2.55mL

1.28mL

25.54mL

5.11mL

2.55mL
参考文献

[1]Cea M, et al. Targeting NAD+ salvage pathway induces autophagy in multiple myeloma cells via mTORC1 and extracellular signal-regulated kinase (ERK1/2) inhibition. Blood. 2012 Oct 25;120(17):3519-29.

[2]Magnone M, et al. NAD+ levels control Ca2+ store replenishment and mitogen-induced increase of cytosolic Ca2+ by Cyclic ADP-ribose-dependent TRPM2 channel gating in human T lymphocytes. J Biol Chem. 2012 Jun 15;287(25):21067-81.

[3]Thakur BK, et al. Inhibition of NAMPT pathway by FK866 activates the function of p53 in HEK293T cells. Biochem Biophys Res Commun. 2012 Aug 3;424(3):371-7.