658084-64-1 | Fk866

Packsize	Purity	Availability	Price	Discounted Price
1mg	98%	in stock	$34.00	$24.00
5mg	98%	in stock	$116.00	$81.00
50mg	98%	in stock	$231.00	$162.00
100mg	98%	in stock	$328.00	$230.00
250mg	98%	in stock	$584.00	$409.00

Description

• Catalog Number: AB48725
• Chemical Name: Fk866
• CAS Number: 658084-64-1
• Molecular Formula: C24H29N3O2
• Molecular Weight: 391.506
• MDL Number: MFCD10565943
• SMILES: O=C(/C=C/c1cccnc1)NCCCCC1CCN(CC1)C(=O)c1ccccc1

Computed Properties

• Complexity: 534
• Covalently-Bonded Unit Count: 1
• Defined Bond Stereocenter Count: 1
• Heavy Atom Count: 29
• Hydrogen Bond Acceptor Count: 3
• Hydrogen Bond Donor Count: 1
• Rotatable Bond Count: 8
• XLogP3: 3.7

Literature

• Inhibition of nicotinamide phosphoribosyltransferase and depletion of nicotinamide adenine dinucleotide contribute to arsenic trioxide suppression of oral squamous cell carcinoma.

  Toxicology and applied pharmacology 20170915

• Retinal toxicity, in vivo and in vitro, associated with inhibition of nicotinamide phosphoribosyltransferase.

  Toxicological sciences : an official journal of the Society of Toxicology 20150301

• On-target effect of FK866, a nicotinamide phosphoribosyl transferase inhibitor, by apoptosis-mediated death in chronic lymphocytic leukemia cells.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20140915

• Elevated microRNA-34a in obesity reduces NAD+ levels and SIRT1 activity by directly targeting NAMPT.

  Aging cell 20131201

• Visfatin is expressed in human granulosa cells: regulation by metformin through AMPK/SIRT1 pathways and its role in steroidogenesis.

  Molecular human reproduction 20130501

• Nicotinamide phosphoribosyl transferase (Nampt) is a target of microRNA-26b in colorectal cancer cells.

  PloS one 20130101

• Synthetic lethality of PARP and NAMPT inhibition in triple-negative breast cancer cells.

  EMBO molecular medicine 20121001

• Inhibition of NAMPT pathway by FK866 activates the function of p53 in HEK293T cells.

  Biochemical and biophysical research communications 20120803

• Role of deleted in breast cancer 1 (DBC1) protein in SIRT1 deacetylase activation induced by protein kinase A and AMP-activated protein kinase.

  The Journal of biological chemistry 20120706

• 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.

  The Journal of biological chemistry 20120615

• Inhibition of nicotinamide phosphoribosyltransferase modifies LPS-induced inflammatory responses of human monocytes.

  Innate immunity 20120601

• Proinflammatory actions of visfatin/nicotinamide phosphoribosyltransferase (Nampt) involve regulation of insulin signaling pathway and Nampt enzymatic activity.

  The Journal of biological chemistry 20120427

• NAMPT pathway is involved in the FOXO3a-mediated regulation of GADD45A expression.

  Biochemical and biophysical research communications 20120420

• The role of sirtuin 2 activation by nicotinamide phosphoribosyltransferase in the aberrant proliferation and survival of myeloid leukemia cells.

  Haematologica 20120401

• Anti-proliferation effect of APO866 on C6 glioblastoma cells by inhibiting nicotinamide phosphoribosyltransferase.

  European journal of pharmacology 20120115

• Pre-B-cell colony-enhancing factor exerts a neuronal protection through its enzymatic activity and the reduction of mitochondrial dysfunction in in vitro ischemic models.

  Journal of neurochemistry 20120101

• Nicotinamide phosphoribosyltransferase: a potent therapeutic target in non-small cell lung cancer with epidermal growth factor receptor-gene mutation.

  Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20120101

• The NAMPT inhibitor FK866 reverts the damage in spinal cord injury.

  Journal of neuroinflammation 20120101

• Overexpression of Nampt in gastric cancer and chemopotentiating effects of the Nampt inhibitor FK866 in combination with fluorouracil.

  Oncology reports 20111101

• Reciprocal potentiation of the antitumoral activities of FK866, an inhibitor of nicotinamide phosphoribosyltransferase, and etoposide or cisplatin in neuroblastoma cells.

  The Journal of pharmacology and experimental therapeutics 20110901

• Suppression of leukocyte infiltration and cartilage degradation by selective inhibition of pre-B cell colony-enhancing factor/visfatin/nicotinamide phosphoribosyltransferase: Apo866-mediated therapy in human fibroblasts and murine collagen-induced arthritis.

  Arthritis and rheumatism 20110701

• Design, synthesis and X-ray crystallographic study of NAmPRTase inhibitors as anti-cancer agents.

  European journal of medicinal chemistry 20110401

• Overcoming temozolomide resistance in glioblastoma via dual inhibition of NAD+ biosynthesis and base excision repair.

  Cancer research 20110315

• Synergistic interactions between HDAC and sirtuin inhibitors in human leukemia cells.

  PloS one 20110101

• Potent synergistic interaction between the Nampt inhibitor APO866 and the apoptosis activator TRAIL in human leukemia cells.

  Experimental hematology 20101101

• Inhibition of nicotinamide phosphoribosyltransferase: cellular bioenergetics reveals a mitochondrial insensitive NAD pool.

  The Journal of biological chemistry 20101029

• Nampt/PBEF/visfatin and cancer.

  Cancer biology & therapy 20100715

• A combination of the metabolic enzyme inhibitor APO866 and the immune adjuvant L-1-methyl tryptophan induces additive antitumor activity.

  Experimental biology and medicine (Maywood, N.J.) 20100701

• A preclinical study on the rescue of normal tissue by nicotinic acid in high-dose treatment with APO866, a specific nicotinamide phosphoribosyltransferase inhibitor.

  Molecular cancer therapeutics 20100601

• Safety and efficacy of NAD depleting cancer drugs: results of a phase I clinical trial of CHS 828 and overview of published data.

  Cancer chemotherapy and pharmacology 20100501

• Inhibition of lactate dehydrogenase A induces oxidative stress and inhibits tumor progression.

  Proceedings of the National Academy of Sciences of the United States of America 20100202

• Target enzyme mutations are the molecular basis for resistance towards pharmacological inhibition of nicotinamide phosphoribosyltransferase.

  BMC cancer 20100101

• Crystal structure of Rattus norvegicus Visfatin/PBEF/Nampt in complex with an FK866-based inhibitor.

  Molecules and cells 20090630

• APO866 activity in hematologic malignancies: a preclinical in vitro study.

  Blood 20090604

• Detection and pharmacological modulation of nicotinamide mononucleotide (NMN) in vitro and in vivo.

  Biochemical pharmacology 20090515

• Circadian control of the NAD+ salvage pathway by CLOCK-SIRT1.

  Science (New York, N.Y.) 20090501

• Circadian clock feedback cycle through NAMPT-mediated NAD+ biosynthesis.

  Science (New York, N.Y.) 20090501

• Circadian rhythms. A circadian loop asSIRTs itself.

  Science (New York, N.Y.) 20090501

• The NAD biosynthesis inhibitor APO866 has potent antitumor activity against hematologic malignancies.

  Blood 20090402

• Catastrophic NAD+ depletion in activated T lymphocytes through Nampt inhibition reduces demyelination and disability in EAE.

  PloS one 20090101

• Extracellular Nampt promotes macrophage survival via a nonenzymatic interleukin-6/STAT3 signaling mechanism.

  The Journal of biological chemistry 20081212

• Visfatin: a new player in mesangial cell physiology and diabetic nephropathy.

  American journal of physiology. Renal physiology 20081101

• Weak coupling of ATP hydrolysis to the chemical equilibrium of human nicotinamide phosphoribosyltransferase.

  Biochemistry 20081021

• Synthesis and biological evaluation of isosteric analogues of FK866, an inhibitor of NAD salvage.

  ChemMedChem 20080501

• NAD depletion by FK866 induces autophagy.

  Autophagy 20080401

• Anticancer agent CHS-828 inhibits cellular synthesis of NAD.

  Biochemical and biophysical research communications 20080321

• Characterization of NAD uptake in mammalian cells.

  The Journal of biological chemistry 20080307

• The pharmacokinetics, toxicities, and biologic effects of FK866, a nicotinamide adenine dinucleotide biosynthesis inhibitor.

  Investigational new drugs 20080201

• Nicotinamide adenine dinucleotide metabolism as an attractive target for drug discovery.

  Expert opinion on therapeutic targets 20070501

• Crystal structure of visfatin/pre-B cell colony-enhancing factor 1/nicotinamide phosphoribosyltransferase, free and in complex with the anti-cancer agent FK-866.

  Journal of molecular biology 20060908

• Chemopotentiating effects of a novel NAD biosynthesis inhibitor, FK866, in combination with antineoplastic agents.

  European journal of medical research 20060830

• Molecular basis for the inhibition of human NMPRTase, a novel target for anticancer agents.

  Nature structural & molecular biology 20060701

• Metabolic signatures associated with a NAD synthesis inhibitor-induced tumor apoptosis identified by 1H-decoupled-31P magnetic resonance spectroscopy.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20050501

• FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis.

  Cancer research 20031101

• Antiangiogenic potency of FK866/K22.175, a new inhibitor of intracellular NAD biosynthesis, in murine renal cell carcinoma.

  Anticancer research 20030101