Home DNA Damage/DNA Repair Sirtuin inhibitor Nicotinamide For research use only.

Nicotinamide

Synonyms: Niacinamide, Vitamin PP, Nicotinic acid amide, Vitamin B3, NSC 27452,NSC 13128

Nicotinamide, a water-soluble vitamin, is an active component of coenzymes NAD and NADP, and also act as an inhibitor of sirtuins.

Nicotinamide Chemical Structure

Nicotinamide Chemical Structure

CAS No. 98-92-0

Purity & Quality Control

Nicotinamide Related Products

Signaling Pathway

Sirtuin Signaling Pathways

Sirtuin Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BL21 (DE3) Function assay Inhibition of catalytically active human SIRT3 (102 to 399 amino acids) expressed in Escherichia coli BL21 (DE3) cells using fluorogenic 7-amino-4-methylcoumarin (AMC)-labeled peptide by fluorescence assay, IC50=6.2μM. 25275824
BL21 (DE3) Function assay Inhibition of full length human SIRT2 expressed in Escherichia coli BL21 (DE3) cells using fluorogenic 7-amino-4-methylcoumarin (AMC)-labeled peptide by fluorescence assay, IC50=10.5μM. 25275824
BL21(DE3) Function assay Inhibition of recombinant Schistosoma mansoni sirtuin 2 (21 to 322 residues) expressed in Escherichia coli BL21(DE3) cells assessed as inhibition of substrate deacetylation using ZMAL as substrate, IC50=23.1μM. 31496251
SK-MEL-28 Function assay 100 uM 24 hrs Reduction in ATP level in human SK-MEL-28 cells at 100 uM maintained in Locke's solution after 24 hrs by luciferase-based assay in absence of GF and glucose 22835719
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
BL21(DE3) Function assay Inhibition of recombinant Schistosoma mansoni sirtuin 2 (21 to 322 residues) expressed in Escherichia coli BL21(DE3) cells in presence of ZMAL 31496251
BL21(DE3) Function assay Inhibition of recombinant Schistosoma mansoni sirtuin 2 (21 to 322 residues) expressed in Escherichia coli BL21(DE3) cells in presence of (Z)-(But)Lys-AMC 31496251
BL21(DE3) Function assay Inhibition of recombinant Schistosoma mansoni sirtuin 2 (21 to 322 residues) expressed in Escherichia coli BL21(DE3) cells in presence of (Z)-(Hex)Lys-AMC 31496251
BL21(DE3) Function assay Inhibition of recombinant Schistosoma mansoni sirtuin 2 (21 to 322 residues) expressed in Escherichia coli BL21(DE3) cells in presence of (Z)-(Oct)Lys-AMC 31496251
HEK293T Function assay 60 mins Inhibition of StrepTag-tagged human SARM1 TIR (561 to 724 residues) expressed in HEK293T cells assessed as reduction in NADase activity in presence of NAD+ incubated for 60 mins by HPLC analysis, IC50=43.8μM. ChEMBL
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Biological Activity

Description Nicotinamide, a water-soluble vitamin, is an active component of coenzymes NAD and NADP, and also act as an inhibitor of sirtuins.
Targets
Sirtuin [1]
In vitro
In vitro

Nicotinamide strongly inhibits yeast silencing, increases rDNA recombination, and shortens replicative life span to that of a sir2 mutant. Nicotinamide abolishes silencing and leads to an eventual delocalization of Sir2 even in G(1)-arrested cells, demonstrating that silent heterochromatin requires continual Sir2 activity. [1] Nicotinamide results in a twofold increase in DNA content and a threefold increase in insulin content in the fetal cells. Nicotinamide induces differentiation and maturation of human fetal pancreatic islet cells. [2] Nicotinamide regulates sirtuins by switching between deacetylation and base exchange. Nicotinamide switching is quantitated for the Sir2s from Archeaglobus fulgidus (Sir2Af2), Saccharomyces cerevisiae (Sir2p), and mouse (Sir2alpha). [3] Nicotinamide selectively reduces a specific phospho-species of tau (Thr231) that is associated with microtubule depolymerization in Alzheimer's disease transgenic mice, in a manner similar to inhibition of SirT1. Nicotinamide also dramatically increases acetylated alpha-tubulin, a primary substrate of SirT2, and MAP2c in Alzheimer's disease transgenic mice, both of which are linked to increased microtubule stability. [4] Nicotinamide fosters DNA integrity and maintains phosphatidylserine membrane asymmetry to prevent cellular inflammation, cellular phagocytosis and vascular thrombosis. Nicotinamide both prevents and reverses neuronal and vascular cell injury. [5]
Cell Research Cell lines HaCaT cells
Concentrations 33 μM
Incubation Time 7 days and 14 days
Method

The established cell line of human epidermal keratinocytes (HaCaT cells) was routinely cultured in Dulbecco's modified Eagle medium (DMEM) containing 10% fetal bovine serum and kept in a humidified atmosphere containing 5% CO2 at 37°C. For NAD(P) modulation, cells were grown in DMEM and 10% dialyzed fetal bovine serum and with addition of 33 μM nicotinamide (33 μM Nam) or without added nicotinamide (0 μM Nam). Cell number was measured by counting. Sensitivity to glutaminase inhibition was performed using 0.1 μM 6-diazo-5-oxo-L-norleucine (DON) on cells grown in 33 μM Nam or 0 μM Nam for 7 days.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-MLC / MLC / p-MYPT1 / MYPT1 p-β-catenin / β-catenin Sp1 / ERK 30503259
Immunofluorescence p-MLC 30503259
In Vivo
In vivo

In the mouse, nicotinamide given i.p. at doses of 100-500 mg/kg showed biphasic elimination with dose-dependent changes in half-life. The initial half-life increased significantly (P <0.05) from 0.8 to 2 h and the terminal half-life increased from 3.4 to 5.6 h over the dose range studied. Clearance, however, decreased significantly from 0.3 to 0.24 L/kg/h only at the highest dose. Peak concentrations increased in a dose-dependent manner from 1,000 to 4,800 nmol/ml. The bioavailability given via the i.p. as compared with the i. v. route was close to 100%[6].
Animal Research Animal Models Mice (strain CBA/Ht/GyfBSVS)
Dosages 100, 200, 300 and 500 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06280482 Recruiting
Smooth Muscle Dysfunction Syndrome (SMDS)
The University of Texas Health Science Center Houston
 March 6 2024 Phase 1
NCT05938036 Not yet recruiting
Acute Respiratory Distress Syndrome (ARDS)
Aqualung Therapeutics Corp.
 January 14 2024 Phase 2
NCT06249581 Active not recruiting
Chronic Stable Angina
Auxilius Pharma sp.z.o.o.
 November 27 2023 Early Phase 1
NCT06036355 Not yet recruiting
Postoperative Prevention of Tumor
Shanghai Cell Therapy Group Co.Ltd
 September 30 2023 Early Phase 1

Chemical Information & Solubility

Molecular Weight 122.12 Formula

C6H6N2O
CAS No. 98-92-0 SDF Download Nicotinamide SDF
Smiles C1=CC(=CN=C1)C(=O)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 24 mg/mL ( (196.52 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 24 mg/mL

Ethanol : 24 mg/mL


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