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(E)-Daporinad

Catalog No. T2644 CAS 658084-64-1

Synonyms: Daporinad, (E)-N-[4-(1-BENZOYL-PIPERIDIN-4-YL)-BUTYL]-3-PYRIDIN-3-YL-ACRYLAMIDE, APO866, FK866

(E)-Daporinad (FK866) is a small molecule inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase), with potential antineoplastic and antiangiogenic activities.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

(E)-Daporinad, CAS 658084-64-1

Pack Size	Availability	Price/USD
2 mg	In stock	$ 36.00
5 mg	In stock	$ 59.00
10 mg	In stock	$ 97.00
25 mg	In stock	$ 198.00
50 mg	In stock	$ 387.00
100 mg	In stock	$ 587.00
500 mg	In stock	$ 1,230.00
1 mL * 10 mM (in DMSO)	In stock	$ 64.00

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Purity: 100%

Purity: 99.96%

Purity: 99.44%

Purity: 98.62%

Purity: 98.44%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	(E)-Daporinad (FK866) is a small molecule inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase), with potential antineoplastic and antiangiogenic activities.
Targets&IC50	NMPRTase:0.4 nM(Ki)
Kinase Assay	High Throughput Screening: FITC-MBM1 at 15 nM and menin at 150 nM in the FP buffer are mixed and incubated for 1h in the dark at room temperature. For point screening, the 0.2 μL of each compound (20 μM final concentration, 1% DMSO) is added to 20 μL of the aliquot of the protein-peptide mixture and incubated on 384-well plates in the dark at room temperature for 1h. In confirmation screening, the serial dilution plates with compounds in DMSO are prepared and used to titrate the menin-FITC-MBM1 complex. Change in fluorescence polarization is monitored at 525 nm after excitations at 495 nm using the PHERAstar microplate reader (BMG) and applied to determine IC50 values with the Origin 7.0 program.
Cell Research	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)

Synonyms	Daporinad, (E)-N-[4-(1-BENZOYL-PIPERIDIN-4-YL)-BUTYL]-3-PYRIDIN-3-YL-ACRYLAMIDE, APO866, FK866
Molecular Weight	391.51
Formula	C24H29N3O2
CAS No.	658084-64-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 72 mg/mL (183.9 mM)

References and Literature

1. Nahimana A, et al. Blood, 2009, 113(14), 3276-3286. 2. Evans L, et al. Arthritis Rheum, 2011, 63(7), 1866-1877. 3. Olesen UH, et al. Mol Cancer Ther, 2010, 9(6), 1609-1617. 4. Zoppoli G, et al. Exp Hematol, 2010, 38(11), 979-988.

Citations

1. Xu B, Zhang P, Tang X, et al. Metabolic Rewiring of Kynurenine Pathway during Hepatic Ischemia–Reperfusion Injury Exacerbates Liver Damage by Impairing NAD Homeostasis. Advanced Science. 2022: 2204697. 2. Liu H Y, Wang F H, Liang J M, et al. Targeting NAD metabolism regulates extracellular adenosine levels to improve the cytotoxicity of CD8+ effector T cells in the tumor microenvironment of gastric cancer. Journal of Cancer Research and Clinical Oncology. 2022: 1-14

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Inhibitor Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Metabolism Compound Library Anti-Aging Compound Library Bioactive Compound Library Clinical Compound Library Anti-Cancer Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

(E)-Daporinad 658084-64-1 Autophagy Metabolism NAMPT Transferase Daporinad inhibit Visfatin (E)-N-[4-(1-BENZOYL-PIPERIDIN-4-YL)-BUTYL]-3-PYRIDIN-3-YL-ACRYLAMIDE (E) Daporinad FK 866 Nicotinamide phosphoribosyl transferase PBEF APO866 FK866 APO 866 Inhibitor Pre-B cell colony enhancing factor APO-866 (E)Daporinad FK-866 inhibitor

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