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Cat.No.S1899
| Related Targets | HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Casein Kinase eIF |
|---|---|
| Other Sirtuin Products | SRT1720 HCl Selisistat (EX-527) Sirtinol 3-TYP AGK2 OSS_128167 SRT2104 (GSK2245840) SirReal2 Thiomyristoyl Salvianolic acid B |
| 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 | ||
| Click to View More Cell Line Experimental Data | ||||||
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In vitro |
DMSO
: 24 mg/mL
(196.52 mM)
Water : 24 mg/mL Ethanol : 24 mg/mL |
|
In vivo |
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| Molecular Weight | 122.12 | Formula | C6H6N2O |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 98-92-0 | Download SDF | Storage of Stock Solutions |
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| Synonyms | Niacinamide, Vitamin PP, Nicotinic acid amide, Vitamin B3, NSC 27452,NSC 13128 | Smiles | C1=CC(=CN=C1)C(=O)N | ||
| Targets/IC50/Ki |
Sirtuin
|
|---|---|
| In vitro |
Nicotinamide strongly inhibits yeast silencing, increases rDNA recombination, and shortens replicative life span to that of a sir2 mutant. This compound abolishes silencing and leads to an eventual delocalization of Sir2 even in G(1)-arrested cells, demonstrating that silent heterochromatin requires continual Sir2 activity. It results in a twofold increase in DNA content and a threefold increase in insulin content in the fetal cells. This chemical induces differentiation and maturation of human fetal pancreatic islet cells. It regulates sirtuins by switching between deacetylation and base exchange. This switching is quantitated for the Sir2s from Archeaglobus fulgidus (Sir2Af2), Saccharomyces cerevisiae (Sir2p), and mouse (Sir2alpha). The compound 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. It 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. This chemical fosters DNA integrity and maintains phosphatidylserine membrane asymmetry to prevent cellular inflammation, cellular phagocytosis and vascular thrombosis. It both prevents and reverses neuronal and vascular cell injury. |
| 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%. |
References |
|
| Methods | Biomarkers | Images | PMID |
|---|---|---|---|
| Western blot | Sp1 / ERK p-β-catenin / β-catenin p-MLC / MLC / p-MYPT1 / MYPT1 |
|
18446063 |
| Immunofluorescence | p-MLC |
|
30503259 |
(data from https://clinicaltrials.gov, updated on 2024-05-22)
| 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 |
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