FK-866 HCl

SKU: orb1305223

Description

FK866 (Daporinad) is a potent and specific non-competitive inhibitor of NAMPT with an IC50 of 0.09 nM. It is widely used in oncology research to study NAD+ depletion, demonstrating anti-proliferative effects in vitro and anti-tumor activity in various xenograft models.

Research Area

Cell Biology, Epigenetics & Chromatin

Key Properties

• CAS Number: 658084-64-1
• MW: 428.0
• Purity: >98%
• Formula: C₂₄H₂₉N₃O₂ ∙ HCl
• SMILES: C(=O)(N1CCC(CCCCNC(/C=C/C=2C=CC=NC2)=O)CC1)C3=CC=CC=C3
• Target: Energy production
• Solubility: Soluble in Water (up to 40 mg/ml).

Bioactivity

• Target IC50:
  NAMPT:0.09 nM|NMPRTase:0.4 nM (Ki)
• In Vivo:
  METHODS: (E)-Daporinad（ FK866 ）(10 mg/kg, intraperitoneal injection) was administered to mice 24, 12, and 0.5 hours before treatment with GaIN/LPS and ConA to test the potential effect of (E)-Daporinad（ FK866 ） on ALF in mice. RESULTS (E)-Daporinad（ FK866 ） treatment reduced the mortality of mice treated with GaIN/LPS or ConA. (E)-Daporinad（ FK866 ） treatment before and after treatment attenuated GaIN/LPS and ConA-induced ALF in mice, and (E)-Daporinad（ FK866 ） pretreatment resulted in a better response to GaIN/LPS or ConA challenge.
• In Vitro:
  METHODS: Hepatocytes were pretreated with (E)-Daporinad（ FK866 ） (100 nM, 30 minutes) and then challenged with GaIN/LPS (G/L, 1 mg/mL /30 ng/mL, 24 hours) to observe whether (E)-Daporinad（ FK866 ） could alleviate GaIN/LPS-induced hepatotoxicity. RESULTS Primary hepatocytes pretreated with (E)-Daporinad（ FK866 ） showed a significant increase in autophagic activity after GaIN/LPS injury. (E)-Daporinad（ FK866 ） could improve liver injury induced by GaIN/LPS and ConA. Its protective mechanism may involve its ability to induce autophagy by inhibiting JNK.
• 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)

Storage & Handling

• Storage: -20°C (hygroscopic)
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

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

Compound Identifiers

PubChem CID

6914657