CHS-828 (nicotinate)
Based on 4 publication(s) in Google Scholar
CHS-828 nicotinate is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), with an IC50 less than 25 nM. CHS-828 nicotinate (GMX1778) exerts a cytotoxic effect by decreasing the cellular level of NAD+ and exhibits a potent anticancer activity.
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- CAS No.: 1160589-73-0
- Formula: C25H27ClN6O3
- Molecular Weight:494.97
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) CHS-828 (nicotinate)
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Biological Activity
Description
Chemical Information
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CAS No. 1160589-73-0
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Molecular Weight 494.97
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Formula C25H27ClN6O3
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SMILES
N#CN/C(NCCCCCCOC1=CC=C(C=C1)Cl)=N\C2=CC=NC=C2.O=C(C3=CC=CN=C3)O
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Synonyms
GMX1778 (nicotinate)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (4)
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Journal Impact Factor
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Most Recent
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Biochem Pharmacol
Scutellarein ameliorates pulmonary arterial hypertension via sirtuin 1 mediated deacetylation of nicotinamide nucleotide transhydrogenase. [Abstract]2025 Jul:237:116932. PMID: 40189160 -
Clin Transl Sci
Computational drug discovery pipelines identify NAMPT as a therapeutic target in neuroendocrine prostate cancer. [Abstract]2024 Sep;17(9):e70030. PMID: 39295559 -
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Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
[1]. Watson M, et al. The small molecule GMX1778 is a potent inhibitor of NAD+ biosynthesis: strategy for enhanced therapy in nicotinic acid phosphoribosyltransferase 1-deficient tumors. Mol Cell Biol. 2009 Nov;29(21):5872-88. [Content Brief]
[2]. Cerna D, et al. Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) activity by small molecule GMX1778 regulates reactive oxygen species (ROS)-mediated cytotoxicity in a p53- and nicotinic acid phosphoribosyltransferase1 (NAPRT1)-dependent manner. J Biol Chem. 2012 Jun 22;287(26):22408-17. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CHS-828 (nicotinate) Related Classifications
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