Page last updated: 2024-11-08

(3R,5S)-fluvastatin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

(3R,5S)-fluvastatin : A (6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid diastereoisomer in which the stereocentres beta- and delta- to the carboxy group have R and S configuration, respectively. The drug fluvastatin is an equimolar mixture of this compound and its enantiomer. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID446155
CHEBI ID38565
CHEBI ID93160
SCHEMBL ID556754
SCHEMBL ID2846

Synonyms (44)

Synonym
gtpl2951
(e,3r,5s)-7-[3-(4-fluorophenyl)-1-isopropyl-indol-2-yl]-3,5-dihydroxy-hept-6-enoic acid
6-heptenoic acid, 7-[3-(4-fluorophenyl)-1-(1-methylethyl)-1h-indol-2-yl]-3,5-dihydroxy-, (3r,5s,6e)-
(3r,5s,6e)-7-[3-(4-fluorophenyl)-1-(1-methylethyl)-1h-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid
(3r,5s,6e)-7-[3-(4-fluorophenyl)-1-isopropyl-1h-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid
(3r,5s)-fluvastatin
CHEBI:38565 ,
PRESTWICK2_000859
(3r,5s,6e)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1h-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid
(3r,5s,6e)-rel-7-[3-(4-fluorophenyl)-1-(1-methylethyl)-1h-indol-2-yl]-3,5-dihydroxy-6-heptenoic acid
fluvastatin & primycin
HMS2089P06
(e,3r,5s)-7-[3-(4-fluorophenyl)-1-propan-2-ylindol-2-yl]-3,5-dihydroxyhept-6-enoic acid
HMS3259J15
(3r,5s)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1h-indol-2-yl]-3,5-dihydroxyhept-6-enoic acid
155229-75-7
EN300-51915
NCGC00256490-01
tox21_302765
cas-93957-54-1
pharmakon1600-01504911
nsc758896
cas_93957-54-1
bdbm86704
SCHEMBL556754
CCG-213323
DL-108
NC00659
SCHEMBL2846
FJLGEFLZQAZZCD-MCBHFWOFSA-N
(e)-(3r,5s)-7-[3-(4-fluoro-phenyl)-1-isopropyl-1h-indol-2-yl]-3,5-dihydroxy-hept-6-enoic acid
AKOS024258614
(3r,5s,e)-7-(3-(4-fluorophenyl)-1-isopropyl-1h-indol-2-yl)-3,5-dihydroxyhept-6-enoic acid
CHEBI:93160
SR-05000001489-1
(-)-fluvastatin
(+)-3r,5s-fluvastatin sodium salt
Q417942
HY-14664B
BRD-K66296774-001-02-0
CS-0019897
H11963
DTXSID201020962
EN300-21702553
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
(6E)-7-[3-(4-fluorophenyl)-1-(propan-2-yl)-1H-indol-2-yl]-3,5-dihydroxyhept-6-enoic acidA dihydroxy monocarboxylic acid that is N-isopropylindole which is substituted at position 3 by a p-fluorophenyl group and at position 2 by a 6-carboxy-3,5-dihydroxyhex-1-en-1-yl group. It has four possible diastereoisomers.
statin (synthetic)A statin which does not occur naturally and which is not obtained by chemical transformation of a naturally occurring statin.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (25)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
LuciferasePhotinus pyralis (common eastern firefly)Potency79.64070.007215.758889.3584AID1224835
RAR-related orphan receptor gammaMus musculus (house mouse)Potency0.45920.006038.004119,952.5996AID1159521; AID1159523
GLI family zinc finger 3Homo sapiens (human)Potency2.39330.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency7.64350.000221.22318,912.5098AID1259243; AID1259247; AID743035; AID743042; AID743054; AID743063
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency12.19720.013326.981070.7614AID1346978
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency3.46700.000214.376460.0339AID720691; AID720692
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency38.01200.003041.611522,387.1992AID1159552; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency34.89970.000817.505159.3239AID1159527; AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency1.77030.001530.607315,848.9004AID1224841; AID1224848; AID1224849; AID1259401; AID1259403
pregnane X nuclear receptorHomo sapiens (human)Potency38.57080.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency16.33770.000229.305416,493.5996AID1259244; AID743069; AID743075; AID743091
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency25.37020.001019.414170.9645AID743140; AID743191
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency43.64650.023723.228263.5986AID743222
caspase-3Homo sapiens (human)Potency12.19720.013326.981070.7614AID1346978
aryl hydrocarbon receptorHomo sapiens (human)Potency30.09370.000723.06741,258.9301AID743085; AID743122
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency7.69590.001723.839378.1014AID743083
Histone H2A.xCricetulus griseus (Chinese hamster)Potency113.00400.039147.5451146.8240AID1224845
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency26.76320.000323.4451159.6830AID743065; AID743067
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency30.63790.000627.21521,122.0200AID743219
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency7.69590.001557.789015,848.9004AID1259244
Cellular tumor antigen p53Homo sapiens (human)Potency54.48270.002319.595674.0614AID651631
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency7.69590.001551.739315,848.9004AID1259244
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Sodium/bile acid cotransporterHomo sapiens (human)IC50 (µMol)40.00001.00005.92679.6000AID1600823
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Nuclear receptor subfamily 4 group A member 2Homo sapiens (human)EC50 (µMol)1.90000.01002.89125.1000AID1885210
NAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)EC50 (µMol)128.55007.10007.10007.1000AID1726066; AID1726069
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (203)

Processvia Protein(s)Taxonomy
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor subfamily 4 group A member 2Homo sapiens (human)
response to hypoxiaNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
neuron migrationNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
response to amphetamineNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
DNA-templated transcriptionNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
transcription by RNA polymerase IINuclear receptor subfamily 4 group A member 2Homo sapiens (human)
adult locomotory behaviorNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
post-embryonic developmentNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
central nervous system projection neuron axonogenesisNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
habenula developmentNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
cellular response to oxidative stressNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
regulation of dopamine metabolic processNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
dopamine biosynthetic processNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
neuron maturationNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
negative regulation of neuron apoptotic processNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
regulation of respiratory gaseous exchangeNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
fat cell differentiationNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IINuclear receptor subfamily 4 group A member 2Homo sapiens (human)
neuron apoptotic processNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
general adaptation syndromeNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
canonical Wnt signaling pathwayNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
cellular response to corticotropin-releasing hormone stimulusNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
dopaminergic neuron differentiationNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
midbrain dopaminergic neuron differentiationNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
negative regulation of apoptotic signaling pathwayNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
regulation of transcription by RNA polymerase IINuclear receptor subfamily 4 group A member 2Homo sapiens (human)
central nervous system neuron differentiationNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
sodium ion transportSodium/bile acid cotransporterHomo sapiens (human)
response to organic cyclic compoundSodium/bile acid cotransporterHomo sapiens (human)
bile acid and bile salt transportSodium/bile acid cotransporterHomo sapiens (human)
response to nutrient levelsSodium/bile acid cotransporterHomo sapiens (human)
bile acid signaling pathwaySodium/bile acid cotransporterHomo sapiens (human)
response to estrogenSodium/bile acid cotransporterHomo sapiens (human)
response to ethanolSodium/bile acid cotransporterHomo sapiens (human)
symbiont entry into host cellSodium/bile acid cotransporterHomo sapiens (human)
transmembrane transportSodium/bile acid cotransporterHomo sapiens (human)
cellular response to xenobiotic stimulusSodium/bile acid cotransporterHomo sapiens (human)
regulation of bile acid secretionSodium/bile acid cotransporterHomo sapiens (human)
negative regulation of transcription by RNA polymerase IINAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
base-excision repairNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
double-strand break repairNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
chromatin remodelingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
protein deacetylationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
negative regulation of cell population proliferationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
determination of adult lifespanNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
response to UVNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
retrotransposon silencingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
regulation of double-strand break repair via homologous recombinationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
regulation of lipid metabolic processNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
pericentric heterochromatin formationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
subtelomeric heterochromatin formationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
protein destabilizationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of insulin secretionNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of telomere maintenanceNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic processNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
circadian regulation of gene expressionNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
negative regulation of transcription elongation by RNA polymerase IINAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
ketone biosynthetic processNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
negative regulation of protein import into nucleusNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
glucose homeostasisNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
regulation of circadian rhythmNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
post-translational protein modificationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of fat cell differentiationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
negative regulation of gluconeogenesisNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
negative regulation of gene expression, epigeneticNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
negative regulation of glycolytic processNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
negative regulation of glucose importNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of protein export from nucleusNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of fibroblast proliferationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
regulation of protein secretionNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
regulation of lipid catabolic processNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
protein delipidationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
cardiac muscle cell differentiationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of cold-induced thermogenesisNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
negative regulation of protein localization to chromatinNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of protein localization to chromatinNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
DNA repair-dependent chromatin remodelingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of stem cell population maintenanceNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of chondrocyte proliferationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
regulation of protein localization to plasma membraneNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of blood vessel branchingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of vascular endothelial cell proliferationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
protein localization to site of double-strand breakNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of stem cell proliferationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of stem cell differentiationNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
negative regulation of cellular senescenceNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
positive regulation of double-strand break repairNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (61)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
DNA bindingNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
nuclear receptor activityNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
protein bindingNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
beta-catenin bindingNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
zinc ion bindingNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
nuclear retinoid X receptor bindingNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
protein heterodimerization activityNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
nuclear glucocorticoid receptor bindingNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
virus receptor activitySodium/bile acid cotransporterHomo sapiens (human)
protein bindingSodium/bile acid cotransporterHomo sapiens (human)
bile acid:sodium symporter activitySodium/bile acid cotransporterHomo sapiens (human)
chromatin bindingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
damaged DNA bindingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD+ ADP-ribosyltransferase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
protein bindingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
zinc ion bindingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
nucleotidyltransferase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD-dependent histone deacetylase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
chromatin DNA bindingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
nucleosome bindingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD-dependent protein lysine deacetylase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
protein homodimerization activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD-dependent histone H3K9 deacetylase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD+ bindingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD-dependent histone H3K18 deacetylase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD+-protein-arginine ADP-ribosyltransferase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
DNA damage sensor activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD-dependent histone H3K56 deacetylase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD-dependent protein demyristoylase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD-dependent protein depalmitoylase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD+- protein-lysine ADP-ribosyltransferase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
TORC2 complex bindingNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
NAD+-protein ADP-ribosyltransferase activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
transcription corepressor activityNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (26)

Processvia Protein(s)Taxonomy
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
nucleusNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
nucleoplasmNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
cytoplasmNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
nuclear speckNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
chromatinNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
protein-containing complexNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
transcription regulator complexNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
nucleusNuclear receptor subfamily 4 group A member 2Homo sapiens (human)
plasma membraneSodium/bile acid cotransporterHomo sapiens (human)
basolateral plasma membraneSodium/bile acid cotransporterHomo sapiens (human)
nucleolusNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
nucleusNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
pericentric heterochromatinNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
endoplasmic reticulumNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
site of double-strand breakNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
site of DNA damageNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
nucleusNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
nucleoplasmNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
intracellular membrane-bounded organelleNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
chromosome, subtelomeric regionNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
chromatinNAD-dependent protein deacetylase sirtuin-6Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (29)

Assay IDTitleYearJournalArticle
AID1726071Inhibition of N-terminal His-tagged human recombinant SIRT2 (55 to 356 residues) expressed in Escherichia coli Rossetta2 cells assessed as decrease in substrate deacetylation activity using QPK(acetyl-K) as substrate at 250 to 1000 uM incubated for 30 min2020ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
Structural Basis for Activation of Human Sirtuin 6 by Fluvastatin.
AID1885210Agonist activity at human Nurr1 measured by Gal4-Nurr1 hybrid reporter gene assay2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Medicinal Chemistry and Chemical Biology of Nurr1 Modulators: An Emerging Strategy in Neurodegeneration.
AID1726069Activation of N-terminal His-tagged human SIRT6 (1 to 355 residues) expressed in Escherichia coli M15(pREP4) assessed as increase in deacetylation activity using acetyl-H3K9 peptide as substrate incubated for 2 hrs in presence of NAD+ by mass spectrometri2020ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
Structural Basis for Activation of Human Sirtuin 6 by Fluvastatin.
AID1698005Ratio of drug level in Wistar Hannover rat blood to plasma administered through iv dosing by LC-MS/MS analysis
AID1698011Fraction unbound in human plasma
AID1698010Hepatic clearance in human administered through iv dosing
AID1697999Dissociation constant, acidic pKa of compound measured up to 18 mins by capillary electrophoresis
AID1726072Inhibition of N-terminal His-tagged human recombinant SIRT3 (118 to 399 residues) expressed in Escherichia coli assessed as decrease in substrate deacetylation using QPK(acetyl-K) as substrate at 250 to 1000 uM incubated for 30 mins by fluorescence based 2020ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
Structural Basis for Activation of Human Sirtuin 6 by Fluvastatin.
AID1600823Inhibition of human recombinant NTCP expressed in CHO cells assessed as reduction in [3H]taurocholate uptake incubated for 2 mins by scintillation counting method2019Bioorganic & medicinal chemistry letters, 10-01, Volume: 29, Issue:19
Design, synthesis and biological evaluation of benzamide derivatives as novel NTCP inhibitors that induce apoptosis in HepG2 cells.
AID1698001Lipophilicity, log D of the compound at pH 7.4 by by shake flask method
AID1698003Fraction unbound in rat plasma
AID1698007Ratio of drug level in human blood to plasma administered through iv dosing by LC-MS/MS analysis
AID1726070Inhibition of N-terminal His-tagged human full length recombinant SIRT1 expressed in Escherichia coli at 250 to 1000 uM by fluorescence based analysis2020ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
Structural Basis for Activation of Human Sirtuin 6 by Fluvastatin.
AID1726075Activation of N-terminal His-tagged human SIRT6 (1 to 355 residues) expressed in Escherichia coli M15(pREP4) assessed as increase in substrate deacetylation activity using FdL1 substrate peptide at 250 to 1000 uM incubated for 1 hr in presence of NAD+ by 2020ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
Structural Basis for Activation of Human Sirtuin 6 by Fluvastatin.
AID1631436Antiviral activity against Dengue virus 2 NGC infected in human A549 cells assessed as reduction in virus replication after 48 hrs by renilla luciferase reporter gene assay2016Journal of medicinal chemistry, 06-23, Volume: 59, Issue:12
The Medicinal Chemistry of Dengue Virus.
AID1698000Apparent permeability in dog MDCKII-LE cells at pH 7.4
AID1726067Activation of N-terminal His-tagged human SIRT6 (1 to 355 residues) expressed in Escherichia coli M15(pREP4) assessed as increase in deacetylation activity using acetyl-H3K9 peptide as substrate incubated for 2 hrs in presence of NAD+ by mass spectrometri2020ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
Structural Basis for Activation of Human Sirtuin 6 by Fluvastatin.
AID1726066Activation of recombinant SIRT6 (unknown origin) using fluoro substrate peptide incubated for 1 hr in presence of NAD by Fluor de Lys assay based fluorometric analysis2020ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
Structural Basis for Activation of Human Sirtuin 6 by Fluvastatin.
AID1726074Activation of His-tagged N-terminal truncated human SIRT6 (13 to 355 residues) expressed in Escherichia coli BL21 (DE3) codon+ cells assessed as increase in deacetylation activity using acetyl-H3K9 peptide as substrate incubated for 2 hrs in presence of N2020ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
Structural Basis for Activation of Human Sirtuin 6 by Fluvastatin.
AID1698008Hepatic clearance in Wistar Hannover rat at 1 mg/kg, iv
AID1726068Activation of N-terminal His-tagged human SIRT6 (1 to 355 residues) expressed in Escherichia coli M15(pREP4) assessed as increase in deacetylation activity using FdL1 substrate peptide incubated for 1 hr in presence of NAD+ by fluorescence assay2020ACS medicinal chemistry letters, Nov-12, Volume: 11, Issue:11
Structural Basis for Activation of Human Sirtuin 6 by Fluvastatin.
AID1346838Rat hydroxymethylglutaryl-CoA reductase (Lanosterol biosynthesis pathway)2001The American journal of cardiology, Mar-08, Volume: 87, Issue:5A
Preclinical and clinical pharmacology of Rosuvastatin, a new 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor.
AID1346838Rat hydroxymethylglutaryl-CoA reductase (Lanosterol biosynthesis pathway)1991Journal of medicinal chemistry, Oct, Volume: 34, Issue:10
Synthesis and biological activity of new HMG-CoA reductase inhibitors. 3. Lactones of 6-phenoxy-3,5-dihydroxyhexanoic acids.
AID1346822Human hydroxymethylglutaryl-CoA reductase (Lanosterol biosynthesis pathway)2005Biochemistry, Sep-06, Volume: 44, Issue:35
Binding thermodynamics of statins to HMG-CoA reductase.
AID1346822Human hydroxymethylglutaryl-CoA reductase (Lanosterol biosynthesis pathway)2003Biochemical Society transactions, Jun, Volume: 31, Issue:Pt 3
Molecular mechanism for inhibition of 3-hydroxy-3-methylglutaryl CoA (HMG-CoA) reductase by rosuvastatin.
AID1346838Rat hydroxymethylglutaryl-CoA reductase (Lanosterol biosynthesis pathway)2009Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15
Application of a 3,3-diphenylpentane skeleton as a multi-template for creation of HMG-CoA reductase inhibitors.
AID1346822Human hydroxymethylglutaryl-CoA reductase (Lanosterol biosynthesis pathway)2001Science (New York, N.Y.), May-11, Volume: 292, Issue:5519
Structural mechanism for statin inhibition of HMG-CoA reductase.
AID1346838Rat hydroxymethylglutaryl-CoA reductase (Lanosterol biosynthesis pathway)1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
HMG-CoA reductase inhibitors: design, synthesis, and biological activity of tetrahydroindazole-substituted 3,5-dihydroxy-6-heptenoic acid sodium salts.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (13)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (15.38)18.2507
2000's5 (38.46)29.6817
2010's3 (23.08)24.3611
2020's3 (23.08)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.12

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.12 (24.57)
Research Supply Index2.64 (2.92)
Research Growth Index4.76 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.12)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (23.08%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other10 (76.92%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]