Daporinad (FK866, APO866)

Catalog No.S2799

Daporinad (FK866, APO866) Chemical Structure

Molecular Weight(MW): 391.51

Daporinad (FK866, APO866) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 of 0.09 nM in a cell-free assay. Phase 1/2.

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Cited by 16 Publications

6 Customer Reviews

  • Bar graph showing the effect of the PBEF inhibitor FK866 on PLB-induced autophagy in PC-3 cells. Data are presented as the mean ± SD of three independent experiments. *P<0.05; **P<0.01; and ***P<0.001 by one-way ANOVA.

    Drug Des Devel Ther, 2015, 9: 1511-54. Daporinad (FK866, APO866) purchased from Selleck.

  • Effect of metabolic inhibitors on SRC-1 protein levels. A549 cells grown in glucose-containing medium were treated with NAM or FK866 at the indicated concentration.

    Mol Endocrinol 2014 28(3), 395-405. Daporinad (FK866, APO866) purchased from Selleck.

  • Paraffin-embedded tumor sections derived from MiaPaCa-2 were stained with H&E or anti-Ki67 antibodies (Scale bar: 100 μm); apoptotic cells were visualized by TUNEL staining (green) and counterstained with DAPI (blue) (Scale bar: 10 μm). The proliferation index and apoptotic index in tumor sections were also quantified. These animal experiments were repeated once (n = 5mice per treatment group).

    Cancer Lett, 2016, 379(1):1-11.. Daporinad (FK866, APO866) purchased from Selleck.

  • Immunofluorescence analysis of Aggrecan and Collagen II expression in NP cells.

    Cell Physiol Biochem, 2018, 49(6):2463-2482. Daporinad (FK866, APO866) purchased from Selleck.

  • Inhibition of NAMPT enzymatic activity decreases osteoclast recruitment in the bone remodeling model. FK866‐loaded osmotic pumps were implanted 48 hr before maxillary‐molar extraction. Rats were sacrificed 4 days after tooth extraction. Osteoclast recruitment and activity were analyzed by TRAP enzymatic staining (a) and quantified (b, c and d). N.Oc/BPm: number of TRAP+ osteoclasts per mm of bone surface, Oc.S:BS (%): resorption surface, N.Nc: mean number of nuclei per osteoclast. Magnification ×200. Boxes are delimited by the first and third quartiles (Q1, Q3) and the line shows the median. Outliers are represented by the extreme values, defined as values lower then Q1—1.5 IQR (Inter Quartile Range) or higher then Q3 + 1.5 IQR. (+) represents the mean, *p ≤ 0.05, **p ≤ 0.01 by the Mann-Whitney U-test.

    J Cell Physiol, 2018, 233(9):7402-7414. Daporinad (FK866, APO866) purchased from Selleck.

  • Western blot analysis showing that myelin basic protein (MBP) expression was higher in the NAM group compared to the other three groups at 14 d after stroke induction.

    Neural Plast, 2017, 2017:7019803. Daporinad (FK866, APO866) purchased from Selleck.

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Biological Activity

Description Daporinad (FK866, APO866) effectively inhibits nicotinamide phosphoribosyltransferase (NMPRTase) with IC50 of 0.09 nM in a cell-free assay. Phase 1/2.
Targets
NMPRTase [5]
(Cell-free assay)
0.4 nM(Ki)
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. [1] APO866 at concentration of 10 nM inhibits PBEF-induced secretion of MMP-3, CCL2, and CXCL8 in HFFF2 cells. [2]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human SH-SY5Y cells M{T4bWN6fG:2b4jpZ:Kh[XO|YYm= NGnOenNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUC2VWUXZJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iC2b4ThcEBk\WyudXzhdkBPSURqUDmgcIV3\WxuIFnDOVA:OC53IH7N NHPwXYYyQTl4MUG4Ny=>
human A2780 cells MXzQdo9tcW[ncnH0bY9vKGG|c3H5 NGO2WmI4OiCq NV\1W49JSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{Bi\nSncjC3NkBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiSVO1NF0yKG6P MoXkNlQ1ODV2MUm=
human NYH cells NH\VO3hEgXSxdH;4bYPDqGG|c3H5 M3TOWFMhf2Wna4O= MYXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDOXWgh[2WubIOgZYZ1\XJiMzD3[YVseyCkeTDjcI9vd2enbnnjJJN2en[rdnHsJIF{e2G7LDDJR|UxRTFwNTDuUS=> MoLBNlM3Pzl7MUW=
human HepG2 cells NHPaW2lHfW6ldHnvckBie3OjeR?= M2rhW|EhcA>? MVTJcohq[mm2aX;uJI9nKE6DTWDUJIlvKGi3bXHuJGhmeEd{IHPlcIx{KHW|aX7nJHsyPEOfLX7pZ491cW6jbXnk[U9RWlCSIHHzJJN2[nO2cnH0[UBie3Onc4Pl[EBieyCob4LtZZRqd25ib3[gX|E1S11vbnnjc5RqdmGvaXTlJI1wdm:wdXPs[Y91cWSnIHHmeIVzKDFiaIKgZpkhdGmzdXnkJJNkcW62aXzsZZRqd25iY3;1cpRqdmdiYX7hcJl{cXNuIFnDOVA:Oi5{IH7N Ml\ZNlQyPjRyOE[=
human PC3 cells M3znXWN6fG:2b4jpZ:Kh[XO|YYm= MkiyR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVGM{KGOnbHzzJIJ6KGOub37v[4VvcWNiYYPzZZktKEmFNUC9N{45KG6P MnW5NlQyPjRyOE[=
human A431 cells MlTVR5l1d3SxeHnjxsBie3OjeR?= Mlf1R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVQ{OSClZXzsd{BjgSClbH;uc4dmdmmlIHHzd4F6NCCLQ{WwQVYvOSCwTR?= M3vYc|I1OTZ2MEi2
human K562 cells NXjB[o9nS3m2b4TvfIlkyqCjc4PhfS=> NXO3ZplIQTZiaB?= NGHTUWJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMPTZ{IHPlcIx{KGGodHXyJFk3KGi{czDifUBOXFRiYYPzZZktKEmFNUC9O{4zKG6P MoDnNlM3Pzl7MUW=
human MCF-7 cells MYHDfZRwfG:6aXRCpIF{e2G7 MYi3NkBp NHGzPVBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0ZvNzDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliV2PUMVEh[XO|YYmsJGlEPTB;Nz60JI5O NUTtVWhCOjRzNkSwPFY>
human HCT116 cells M2DiUmN6fG:2b4jpZ:Kh[XO|YYm= M132d|czKGh? NVjzV5dXS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDXV3QuOSCjc4PhfUwhUUN3ME2xNE46KG6P NV;6cItxOjRzNkSwPFY>
human HT1080 cells MmX3R5l1d3SxeHnjxsBie3OjeR?= NUn6foZJPiCmYYnz NWqyWoJrS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUFRzMEiwJINmdGy|IHHmeIVzKDZiZHH5d{BjgSCVUlKgZZN{[XluIFnDOVA:OC5zNjFOwG0> MojjNlE{OzByMUW=
human HCT116 cells MkHMR5l1d3SxeHnjxsBie3OjeR?= NGSxTXk3KGSjeYO= NV3uN3NkS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDZiZHH5d{BjgSCVUlKgZZN{[XluIFnDOVA:OC5zNjFOwG0> Mk\YNlE{OzByMUW=
human A549 cells M4LoPGN6fG:2b4jpZ:Kh[XO|YYm= MWG2JIRigXN? NGDqN5ZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGGodHXyJFYh\GG7czDifUBUWkJiYYPzZZktKEmFNUC9NE4yPiEQvF2= NH;Tfm4zOTN|MECxOS=>
human SNU638 cells NUnkT|JMS3m2b4TvfIlkyqCjc4PhfS=> MUW2JIRigXN? MVHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTUnU3OzhiY3XscJMh[W[2ZYKgOkBl[Xm|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlE3KM7:TR?= NWfQUI5KOjF|M{CwNVU>
human SKOV3 cells M3LmWWN6fG:2b4jpZ:Kh[XO|YYm= M1;RNWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMV1Z|IHPlcIx{KGK7IHPsc45w\2WwaXOgZZN{[XluIFnDOVA:OjFzIH7N NWnLRXl2OjRzNkSwPFY>
human MCF7 cells M3m1WWZ2dmO2aX;uJIF{e2G7 MVuxNEDPxE1? M3X5fVYh\GG7cx?= M1nsT2FvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZZQhOTBidV2gZYZ1\XJiNjDkZZl{KGK7IGPSRkBie3OjeTygTWM2OD1yLk[4JO69VQ>? MWiyNVM{ODBzNR?=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
SIRT1; 

PubMed: 29905535     


Human retinal pigment epithelial cells (ARPE-19) were treated with different doses (0.01-10μM) of FK866 and expression of SIRT1 was evaluated by western blotting.

p-AMPK / AMPK / p-EIF2A / EIF2A / p-4EBP1 / 4EBP1; 

PubMed: 29541451     


CEM PA cells were treated with 5 and 100 nM FK866 for 48 h. Western blot showing expression of AMPK, mTOR, 4EBP1, and EIF2A in CEM PA cells.

AKT / pAKT(Ser-473) / mTOR / p-mTOR(Ser-2448); 

PubMed: 26542945     


Jurkat cells were treated for 48 h with or without (Mock) the indicated concentration of FK866. Thereafter, cells were lysed and the levels of total and p-Akt (Ser-473), total and p-MTOR (Ser-2448), total and p-4EBP1 (Ser-65 and Thr-70).

29905535 29541451 26542945
Immunofluorescence
pMLKL; 

PubMed: 29996103     


Immunofluorescence for pMLKL (monoclonal pMLKL antibody, red, phospho S358) and nuclei (DAPI, blue) in THP-1 cells treated with the indicated concentrations of FK866 for 6 hr. Scale bars, 10 μm. 

phGSK3β; 

PubMed: 22207684     


Representative DUOLINK images of phospho-GSK3β (Ser9) protein expression in HL60 cells treated with 10 nM of FK866 for 96 h or 100 nM of AC93253 for 48 h, or with DMSO as a control.

ph-β-catenin ; 

PubMed: 22207684     


Representative images of inactive phospho-β-catenin (Ser33/37) protein expression in HL60 cells treated with 10 nM of FK866, 100 nM of AC93253 or DMSO as a control

29996103 22207684
Growth inhibition assay
Cell viability ; 

PubMed: 27462772     


Twenty-three PDAC-derived PCCs were treated for 72 h with increasing concentrations of FK866 ranging from 0 to 1000 nM. The horizontal dotted line indicates 50% cell viability. PCCs with the highest sensitivity are highlighted by a blue line and those wit䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ

27462772
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. [1] APO866 at dose of 0.12 mg/kg/hour prevents joint destruction and leukocyte infiltration through inhibition of PBEF in mice with CIA. [2]

Protocol

Cell Research:

[1]
- Collapse
  • Cell lines: 41 hematologic malignant cell lines
  • Concentrations: 0 - 10 nM
  • Incubation Time: 72 hours or 96 hours
  • Method:

    For MTT assays, 0.5 × 106 cells/mL is plated in triplicate on 96-well plates. APO866 (0.01 nM-100 nM) is added in 50 μL of culture medium, with culture medium alone serving as control. After 72 or 96 hours of incubation, 15 μL of dye solution is added to each well and cells are incubated for an additional 4 hours. Stop solution (100 μL/well) is added for 1 hour and the absorbance is read at 570 nm on a spectrophotometer. For trypan blue dye exclusion staining, 0.5 × 105 cells/well is grown in 6-well plates with 1 mL media in the absence or presence of APO866 for 96 hours. Cells from each sample are incubated with 10 μL trypan blue solution (at a 1:1 ratio [vol/vol] for 1 minute). Cell survival is determined by calculating proportion of live (unstained) cells.


    (Only for Reference)
Animal Research:

[1]
- Collapse
  • Animal Models: C.B.-17 SCID mice xenograft models of human AML, lymphoblastic lymphoma, and leukemia.
  • Formulation: 0.9% saline
  • Dosages: 20 mg/kg
  • Administration: administered intraperitoneally twice a day for 4 days, repeated weekly over 3 weeks
    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 78 mg/mL (199.22 mM)
DMSO Insoluble
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O
For best results, use promptly after mixing. 		4mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 391.51
Formula

C24H29N3O2
CAS No. 658084-64-1
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    We are considering the use of S2799 for in vivo injections, Any suggestions for the formula?

  • Answer:

    The vehicle we recommend for S2799 in vivo study is 45% Propylene glycol (dissolve first) +5% Tween 80+ddH2O. You can dissolve the compound in Propylene glycol first and then dilute with water with Tween 80. The solution is clear and can be used for injection.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID