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Literature summary extracted from

  • Yang, L.; He, Y.; Chen, Q.; Qian, S.; Wang, Z.
    Design and synthesis of new 9-substituted norharmane derivatives as potential Sirt5 inhibitors (2017), J. Heterocycl. Chem., 54, 1457-1466 .
No PubMed abstract available

Application

EC Number Application Comment Organism
2.3.1.B43 drug development Sirt5 is a potential drug target for the treatment of cancer, Alzheimer's disease, and Parkinson's disease Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.B43 1-(2-(9H-pyrido[3,4-b]indol-9-yl)ethyl)-3-phenylurea 10% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 3-(((2-(9H-pyrido[3,4-b]indol-9-yl)ethyl)amino)methyl)benzoic acid 32% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 3-((2-(9H-pyrido[3,4-b]indol-9-yl)acetamido)methyl)benzoic acid 21% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 3-((2-(9H-pyrido[3,4-b]indol-9-yl)ethyl)carbamoyl)benzoicacid 15% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 3-(3-(2-(9H-pyrido[3,4-b]indol-9-yl)ethyl)ureido)benzoic acid 36% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 4-(((2-(9H-pyrido[3,4-b]indol-9-yl)ethyl)amino)methyl)benzoic acid 22% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 4-((2-(9H-pyrido[3,4-b]indol-9-yl)acetamido)methyl)benzoic acid 25% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 4-((2-(9H-pyrido[3,4-b]indol-9-yl)ethyl)carbamoyl)benzoic acid 25% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 4-(3-(2-(9H-pyrido[3,4-b]indol-9-yl)ethyl)ureido)benzoic acid 52% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 5-[[4-(benzyloxy)phenyl]methylidene]-2-sulfanylidene-1,3-diazinane-4,6-dione
-
 Homo sapiens
2.3.1.B43 cambinol
-
 Homo sapiens
2.3.1.B43 ethyl 4-[[2-(9H-pyrido[3,4-b]indol-9-yl)acetamido]methyl]benzoate 12% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 GW5074 85% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 additional information design and synthesis of 9-substituted norharmane derivatives as potential Sirt5 inhibitors, molceular docking, overview Homo sapiens
2.3.1.B43 N-(2-(9H-pyrido[3,4-b]indol-9-yl)ethyl)benzamide 7% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 N-(4-chlorobenzyl)-2-(9H-pyrido[3,4-b]indol-9-yl)acetamide 18% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 N-(pyridin-3-ylmethyl)-2-(9H-pyrido[3,4-b]indol-9-yl)acetamide 24% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 N-benzyl-2-(9H-pyrido[3,4-b]indol-9-yl)acetamide 8% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 N-benzyl-2-(9H-pyrido[3,4-b]indol-9-yl)ethan-1-amine 10% inhibition at 0.1 mM Homo sapiens
2.3.1.B43 nicotinamide
-
 Homo sapiens
2.3.1.B43 sirtinol
-
 Homo sapiens
2.3.1.B43 suramin
-
 Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
2.3.1.B43 mitochondrion
-
 Homo sapiens 5739
-

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.B43 Homo sapiens Q9NXA8
-
-

Synonyms

EC Number Synonyms Comment Organism
2.3.1.B43 SIRT5
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.B43 0.0126
-
 pH and temperature not specified in the publication Homo sapiens 5-[[4-(benzyloxy)phenyl]methylidene]-2-sulfanylidene-1,3-diazinane-4,6-dione
2.3.1.B43 0.0425
-
 pH and temperature not specified in the publication Homo sapiens cambinol
2.3.1.B43 0.0466
-
 pH and temperature not specified in the publication Homo sapiens nicotinamide
2.3.1.B43 0.0466
-
 pH and temperature not specified in the publication Homo sapiens suramin
2.3.1.B43 0.0489
-
 pH and temperature not specified in the publication Homo sapiens sirtinol

General Information

EC Number General Information Comment Organism
2.3.1.B43 malfunction because these modifications by Sirt5 cover a broad range of pivotal protein substrates involved in cellular metabolism and metabolic energy homeostasis, aberrant activity of Sirt5 is considered to be a very critical factor for many human diseases, for example, cancer, Alzheimer's disease, and Parkinson's disease Homo sapiens
2.3.1.B43 physiological function Sirt5 has only weak deacetylation, but has robust desuccinylation, demalonylation, and deglutarylation activities in vitro and in vivo. Modifications by Sirt5 cover a broad range of pivotal protein substrates involved in cellular metabolism and metabolic energy homeostasis Homo sapiens