Page last updated: 2024-11-13

2-(3,4-dimethoxyphenyl)-1-(5-methoxy-2,2-dimethyl-2h-chromen-6-yl)ethanone

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

Description

The compound you've described is **2-(3,4-dimethoxyphenyl)-1-(5-methoxy-2,2-dimethyl-2H-chromen-6-yl)ethanone**. It's a complex organic molecule, but let's break it down:

* **2-(3,4-dimethoxyphenyl):** This part indicates a phenyl ring (a six-membered carbon ring with alternating double bonds) with two methoxy groups (CH3O-) attached at positions 3 and 4 on the ring.
* **-1-(5-methoxy-2,2-dimethyl-2H-chromen-6-yl):** This part describes a chromene ring system.
* **2H-chromen:** This refers to a chromene ring (a six-membered ring with a fused five-membered ring containing oxygen) where the hydrogen on position 2 has been replaced by a substituent.
* **2,2-dimethyl:** Two methyl groups (CH3-) are attached at position 2 on the chromene ring.
* **5-methoxy:** A methoxy group is attached at position 5 on the chromene ring.
* **6-yl:** This signifies that the chromene ring is attached to another group at position 6.
* **ethanone:** This is a ketone group (-COCH3) attached to the chromene ring.

**Importance in Research:**

The specific importance of this compound depends on the context of its research. However, its structure suggests potential uses in a few areas:

* **Pharmacology/Medicinal Chemistry:** Compounds with chromene ring systems are often found to have biological activity, including anti-inflammatory, anti-cancer, and anti-microbial properties. The methoxy groups and the phenyl ring could further enhance these properties by influencing how the compound interacts with biological targets.
* **Material Science:** Chromene derivatives are sometimes used in the synthesis of polymers, dyes, and other materials. The specific arrangement of functional groups in this molecule could give rise to unique properties relevant to these applications.

**To understand the specific importance of this compound, you would need more context about the research it's involved in.** For example:

* **What research question is being addressed?**
* **What are the specific biological targets or applications being studied?**
* **What are the experimental results obtained with this compound?**

If you can provide more information about the research context, I can help you better understand why this specific compound is being investigated.

2-(3,4-dimethoxyphenyl)-1-(5-methoxy-2,2-dimethyl-2H-chromen-6-yl)ethanone: an Hsp90 inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID71453910
CHEMBL ID2177146
SCHEMBL ID16694242
MeSH IDM0582019

Synonyms (6)

Synonym
CHEMBL2177146 ,
SCHEMBL16694242
2-(3,4-dimethoxyphenyl)-1-(5-methoxy-2,2-dimethyl-2h-chromen-6-yl)ethanone
TZRPLTHVBYHDBJ-UHFFFAOYSA-N
bdbm50459690
PD174438

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Taken together, our findings illustrate the superior properties of SH-1242 as an Hsp90 inhibitor and as an effective antitumor and minimally toxic agent, providing a foundation for advancing further preclinical and clinical studies."( Deguelin Analogue SH-1242 Inhibits Hsp90 Activity and Exerts Potent Anticancer Efficacy with Limited Neurotoxicity.
An, H; Bae, SY; Choi, H; Hyun, SY; Kim, JY; Kim, KW; Kim, YM; Lee, HJ; Lee, HY; Lee, J; Lee, S; Lee, SC; Lee, SK; Min, HY; Moon, J; Park, HJ; Park, KH; Park, SH; Park, SJ; Seo, JH; Suh, YG, 2016
)
0.43
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Heat shock protein HSP 90-alphaHomo sapiens (human)IC50 (µMol)0.09000.00040.695010.0000AID1543588
Hypoxia-inducible factor 1-alphaHomo sapiens (human)IC50 (µMol)2.15000.00072.46529.2100AID1387506
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (123)

Processvia Protein(s)Taxonomy
telomere maintenance via telomeraseHeat shock protein HSP 90-alphaHomo sapiens (human)
neuron migrationHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of protein phosphorylationHeat shock protein HSP 90-alphaHomo sapiens (human)
activation of innate immune responseHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of defense response to virus by hostHeat shock protein HSP 90-alphaHomo sapiens (human)
skeletal muscle contractionHeat shock protein HSP 90-alphaHomo sapiens (human)
mitochondrial transportHeat shock protein HSP 90-alphaHomo sapiens (human)
response to unfolded proteinHeat shock protein HSP 90-alphaHomo sapiens (human)
response to heatHeat shock protein HSP 90-alphaHomo sapiens (human)
response to coldHeat shock protein HSP 90-alphaHomo sapiens (human)
response to xenobiotic stimulusHeat shock protein HSP 90-alphaHomo sapiens (human)
response to salt stressHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of lamellipodium assemblyHeat shock protein HSP 90-alphaHomo sapiens (human)
cardiac muscle cell apoptotic processHeat shock protein HSP 90-alphaHomo sapiens (human)
regulation of protein ubiquitinationHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of protein polymerizationHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of interferon-beta productionHeat shock protein HSP 90-alphaHomo sapiens (human)
regulation of protein localizationHeat shock protein HSP 90-alphaHomo sapiens (human)
protein refoldingHeat shock protein HSP 90-alphaHomo sapiens (human)
response to cocaineHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of protein import into nucleusHeat shock protein HSP 90-alphaHomo sapiens (human)
regulation of apoptotic processHeat shock protein HSP 90-alphaHomo sapiens (human)
regulation of protein-containing complex assemblyHeat shock protein HSP 90-alphaHomo sapiens (human)
protein unfoldingHeat shock protein HSP 90-alphaHomo sapiens (human)
response to estrogenHeat shock protein HSP 90-alphaHomo sapiens (human)
protein insertion into mitochondrial outer membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of nitric oxide biosynthetic processHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of protein catabolic processHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of cell sizeHeat shock protein HSP 90-alphaHomo sapiens (human)
response to antibioticHeat shock protein HSP 90-alphaHomo sapiens (human)
protein stabilizationHeat shock protein HSP 90-alphaHomo sapiens (human)
chaperone-mediated protein complex assemblyHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of cardiac muscle contractionHeat shock protein HSP 90-alphaHomo sapiens (human)
chaperone-mediated autophagyHeat shock protein HSP 90-alphaHomo sapiens (human)
cellular response to virusHeat shock protein HSP 90-alphaHomo sapiens (human)
regulation of postsynaptic membrane neurotransmitter receptor levelsHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of tau-protein kinase activityHeat shock protein HSP 90-alphaHomo sapiens (human)
telomerase holoenzyme complex assemblyHeat shock protein HSP 90-alphaHomo sapiens (human)
cellular response to heatHeat shock protein HSP 90-alphaHomo sapiens (human)
protein foldingHeat shock protein HSP 90-alphaHomo sapiens (human)
positive regulation of chemokine-mediated signaling pathwayHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of signaling receptor activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
response to hypoxiaHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of DNA-templated transcriptionHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIHypoxia-inducible factor 1-alphaHomo sapiens (human)
response to reactive oxygen speciesHypoxia-inducible factor 1-alphaHomo sapiens (human)
angiogenesisHypoxia-inducible factor 1-alphaHomo sapiens (human)
response to hypoxiaHypoxia-inducible factor 1-alphaHomo sapiens (human)
intracellular glucose homeostasisHypoxia-inducible factor 1-alphaHomo sapiens (human)
neural crest cell migrationHypoxia-inducible factor 1-alphaHomo sapiens (human)
epithelial to mesenchymal transitionHypoxia-inducible factor 1-alphaHomo sapiens (human)
embryonic placenta developmentHypoxia-inducible factor 1-alphaHomo sapiens (human)
B-1 B cell homeostasisHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of endothelial cell proliferationHypoxia-inducible factor 1-alphaHomo sapiens (human)
heart loopingHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of neuroblast proliferationHypoxia-inducible factor 1-alphaHomo sapiens (human)
chondrocyte differentiationHypoxia-inducible factor 1-alphaHomo sapiens (human)
glandular epithelial cell maturationHypoxia-inducible factor 1-alphaHomo sapiens (human)
connective tissue replacement involved in inflammatory response wound healingHypoxia-inducible factor 1-alphaHomo sapiens (human)
outflow tract morphogenesisHypoxia-inducible factor 1-alphaHomo sapiens (human)
cardiac ventricle morphogenesisHypoxia-inducible factor 1-alphaHomo sapiens (human)
lactate metabolic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of glycolytic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of DNA-templated transcriptionHypoxia-inducible factor 1-alphaHomo sapiens (human)
intracellular iron ion homeostasisHypoxia-inducible factor 1-alphaHomo sapiens (human)
signal transductionHypoxia-inducible factor 1-alphaHomo sapiens (human)
neuroblast proliferationHypoxia-inducible factor 1-alphaHomo sapiens (human)
lactationHypoxia-inducible factor 1-alphaHomo sapiens (human)
visual learningHypoxia-inducible factor 1-alphaHomo sapiens (human)
response to iron ionHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of gene expressionHypoxia-inducible factor 1-alphaHomo sapiens (human)
vascular endothelial growth factor productionHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of vascular endothelial growth factor productionHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of gene expressionHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of gene expressionHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of epithelial cell migrationHypoxia-inducible factor 1-alphaHomo sapiens (human)
response to muscle activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
axonal transport of mitochondrionHypoxia-inducible factor 1-alphaHomo sapiens (human)
neural fold elevation formationHypoxia-inducible factor 1-alphaHomo sapiens (human)
cerebral cortex developmentHypoxia-inducible factor 1-alphaHomo sapiens (human)
bone mineralizationHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of bone mineralizationHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of vascular endothelial growth factor receptor signaling pathwayHypoxia-inducible factor 1-alphaHomo sapiens (human)
TOR signalingHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of TOR signalingHypoxia-inducible factor 1-alphaHomo sapiens (human)
intracellular oxygen homeostasisHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of chemokine productionHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of transforming growth factor beta2 productionHypoxia-inducible factor 1-alphaHomo sapiens (human)
collagen metabolic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
cellular response to oxidative stressHypoxia-inducible factor 1-alphaHomo sapiens (human)
embryonic hemopoiesisHypoxia-inducible factor 1-alphaHomo sapiens (human)
insulin secretion involved in cellular response to glucose stimulusHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of insulin secretion involved in cellular response to glucose stimulusHypoxia-inducible factor 1-alphaHomo sapiens (human)
hemoglobin biosynthetic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of blood vessel endothelial cell migrationHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of erythrocyte differentiationHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of angiogenesisHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of DNA-templated transcriptionHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of growthHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIHypoxia-inducible factor 1-alphaHomo sapiens (human)
muscle cell cellular homeostasisHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of hormone biosynthetic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
digestive tract morphogenesisHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of nitric-oxide synthase activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
neuron apoptotic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
elastin metabolic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
intestinal epithelial cell maturationHypoxia-inducible factor 1-alphaHomo sapiens (human)
epithelial cell differentiation involved in mammary gland alveolus developmentHypoxia-inducible factor 1-alphaHomo sapiens (human)
iris morphogenesisHypoxia-inducible factor 1-alphaHomo sapiens (human)
retina vasculature development in camera-type eyeHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of thymocyte apoptotic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
cellular response to interleukin-1Hypoxia-inducible factor 1-alphaHomo sapiens (human)
cellular response to hypoxiaHypoxia-inducible factor 1-alphaHomo sapiens (human)
dopaminergic neuron differentiationHypoxia-inducible factor 1-alphaHomo sapiens (human)
mesenchymal cell apoptotic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
hypoxia-inducible factor-1alpha signaling pathwayHypoxia-inducible factor 1-alphaHomo sapiens (human)
cellular response to virusHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of cytokine production involved in inflammatory responseHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of mitophagyHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of miRNA transcriptionHypoxia-inducible factor 1-alphaHomo sapiens (human)
positive regulation of miRNA transcriptionHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of oxidative stress-induced neuron intrinsic apoptotic signaling pathwayHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of aerobic respirationHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of reactive oxygen species metabolic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of protein neddylationHypoxia-inducible factor 1-alphaHomo sapiens (human)
negative regulation of mesenchymal cell apoptotic processHypoxia-inducible factor 1-alphaHomo sapiens (human)
regulation of transcription by RNA polymerase IIHypoxia-inducible factor 1-alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (48)

Processvia Protein(s)Taxonomy
UTP bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
CTP bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
RNA bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
mRNA bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
protein bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
ATP bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
GTP bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
ATP hydrolysis activityHeat shock protein HSP 90-alphaHomo sapiens (human)
sulfonylurea receptor bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
protein phosphatase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
MHC class II protein complex bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
nitric-oxide synthase regulator activityHeat shock protein HSP 90-alphaHomo sapiens (human)
TPR domain bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
ubiquitin protein ligase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
dATP bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
identical protein bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
protein homodimerization activityHeat shock protein HSP 90-alphaHomo sapiens (human)
histone deacetylase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
transmembrane transporter bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
tau protein bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
GTPase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
Rho GDP-dissociation inhibitor bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
DNA polymerase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
scaffold protein bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
disordered domain specific bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
ATP-dependent protein folding chaperoneHeat shock protein HSP 90-alphaHomo sapiens (human)
protein tyrosine kinase bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
unfolded protein bindingHeat shock protein HSP 90-alphaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificHypoxia-inducible factor 1-alphaHomo sapiens (human)
sequence-specific DNA bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificHypoxia-inducible factor 1-alphaHomo sapiens (human)
cis-regulatory region sequence-specific DNA bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
DNA-binding transcription activator activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
DNA-binding transcription repressor activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
transcription coactivator bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificHypoxia-inducible factor 1-alphaHomo sapiens (human)
p53 bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
DNA-binding transcription factor activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
protein bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
nuclear receptor bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
enzyme bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
protein kinase bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
protein domain specific bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
ubiquitin protein ligase bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
histone deacetylase bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
protein heterodimerization activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
Hsp90 protein bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
E-box bindingHypoxia-inducible factor 1-alphaHomo sapiens (human)
transcription regulator activator activityHypoxia-inducible factor 1-alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (34)

Processvia Protein(s)Taxonomy
extracellular regionHeat shock protein HSP 90-alphaHomo sapiens (human)
nucleusHeat shock protein HSP 90-alphaHomo sapiens (human)
nucleoplasmHeat shock protein HSP 90-alphaHomo sapiens (human)
cytoplasmHeat shock protein HSP 90-alphaHomo sapiens (human)
mitochondrionHeat shock protein HSP 90-alphaHomo sapiens (human)
cytosolHeat shock protein HSP 90-alphaHomo sapiens (human)
plasma membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
cell surfaceHeat shock protein HSP 90-alphaHomo sapiens (human)
membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
basolateral plasma membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
apical plasma membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
brush border membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
secretory granule lumenHeat shock protein HSP 90-alphaHomo sapiens (human)
melanosomeHeat shock protein HSP 90-alphaHomo sapiens (human)
neuronal cell bodyHeat shock protein HSP 90-alphaHomo sapiens (human)
lysosomal lumenHeat shock protein HSP 90-alphaHomo sapiens (human)
dendritic growth coneHeat shock protein HSP 90-alphaHomo sapiens (human)
axonal growth coneHeat shock protein HSP 90-alphaHomo sapiens (human)
perinuclear region of cytoplasmHeat shock protein HSP 90-alphaHomo sapiens (human)
collagen-containing extracellular matrixHeat shock protein HSP 90-alphaHomo sapiens (human)
extracellular exosomeHeat shock protein HSP 90-alphaHomo sapiens (human)
endocytic vesicle lumenHeat shock protein HSP 90-alphaHomo sapiens (human)
sperm mitochondrial sheathHeat shock protein HSP 90-alphaHomo sapiens (human)
sperm plasma membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
ficolin-1-rich granule lumenHeat shock protein HSP 90-alphaHomo sapiens (human)
protein-containing complexHeat shock protein HSP 90-alphaHomo sapiens (human)
plasma membraneHeat shock protein HSP 90-alphaHomo sapiens (human)
neuronal cell bodyHeat shock protein HSP 90-alphaHomo sapiens (human)
perinuclear region of cytoplasmHeat shock protein HSP 90-alphaHomo sapiens (human)
myelin sheathHeat shock protein HSP 90-alphaHomo sapiens (human)
cytosolHeat shock protein HSP 90-alphaHomo sapiens (human)
nucleusHeat shock protein HSP 90-alphaHomo sapiens (human)
nucleusHypoxia-inducible factor 1-alphaHomo sapiens (human)
nucleoplasmHypoxia-inducible factor 1-alphaHomo sapiens (human)
cytoplasmHypoxia-inducible factor 1-alphaHomo sapiens (human)
cytosolHypoxia-inducible factor 1-alphaHomo sapiens (human)
nuclear bodyHypoxia-inducible factor 1-alphaHomo sapiens (human)
nuclear speckHypoxia-inducible factor 1-alphaHomo sapiens (human)
motile ciliumHypoxia-inducible factor 1-alphaHomo sapiens (human)
axon cytoplasmHypoxia-inducible factor 1-alphaHomo sapiens (human)
chromatinHypoxia-inducible factor 1-alphaHomo sapiens (human)
euchromatinHypoxia-inducible factor 1-alphaHomo sapiens (human)
protein-containing complexHypoxia-inducible factor 1-alphaHomo sapiens (human)
RNA polymerase II transcription regulator complexHypoxia-inducible factor 1-alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (25)

Assay IDTitleYearJournalArticle
AID711227Inhibition of HSP90 binding to HIF1alpha in human H1299 cells at 12.5 uM after 30 mins by immunoprecipitation and immunoblotting analysis2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Design, synthesis, and biological evaluation of novel deguelin-based heat shock protein 90 (HSP90) inhibitors targeting proliferation and angiogenesis.
AID711225Antiangiogenic activity in transgenic zebrafish embryos at 50% epiboly after 5.3 hrs2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Design, synthesis, and biological evaluation of novel deguelin-based heat shock protein 90 (HSP90) inhibitors targeting proliferation and angiogenesis.
AID711226Inhibition of HSP90 binding to HIF1alpha in human H1299 cells at 12.5 uM after 30 mins by immunoprecipitation and immunoblotting analysis in presence of ATP2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Design, synthesis, and biological evaluation of novel deguelin-based heat shock protein 90 (HSP90) inhibitors targeting proliferation and angiogenesis.
AID1261571Inhibition of HIF-1alpha in human H1299 cells at 100 nM after 72 hrs subsequently incubated for 12 hrs under hypoxic conditions by Western blot assay relative to control2015European journal of medicinal chemistry, Nov-02, Volume: 104Ring-truncated deguelin derivatives as potent Hypoxia Inducible Factor-1α (HIF-1α) inhibitors.
AID711222Toxicity in transgenic zebrafish embryos assessed as developmental deffect at 50 nM to 1.25 uM after 24 hrs2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Design, synthesis, and biological evaluation of novel deguelin-based heat shock protein 90 (HSP90) inhibitors targeting proliferation and angiogenesis.
AID711218Toxicity in transgenic zebrafish embryos assessed as effect on growth at 50 nM to 1.25 uM after 74 hrs2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Design, synthesis, and biological evaluation of novel deguelin-based heat shock protein 90 (HSP90) inhibitors targeting proliferation and angiogenesis.
AID711223Toxicity in transgenic zebrafish embryos assessed as developmental deffect at 10 uM after 24 hrs2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Design, synthesis, and biological evaluation of novel deguelin-based heat shock protein 90 (HSP90) inhibitors targeting proliferation and angiogenesis.
AID711215Toxicity in transgenic zebrafish embryos assessed as effect on viability at 50 nM to 1.25 uM after 74 hrs2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Design, synthesis, and biological evaluation of novel deguelin-based heat shock protein 90 (HSP90) inhibitors targeting proliferation and angiogenesis.
AID1387506Inhibition of HIF-1alpha in human HRE-A549 cells pre-incubated for 1 hr before exposure to hypoxia for 24 hrs by HRE-luciferase reporter gene assay2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Novel Hypoxia-Inducible Factor 1α (HIF-1α) Inhibitors for Angiogenesis-Related Ocular Diseases: Discovery of a Novel Scaffold via Ring-Truncation Strategy.
AID1543584Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth at 10 uM after 72 hrs by MTT assay relative to control2019European journal of medicinal chemistry, Apr-01, Volume: 167Design, synthesis, and biological evaluation of truncated deguelin derivatives as Hsp90 inhibitors.
AID708845Cytotoxicity against human H1299 cells after 3 days by MTS assay2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Design, synthesis, and biological evaluation of novel deguelin-based heat shock protein 90 (HSP90) inhibitors targeting proliferation and angiogenesis.
AID1387519Suppression of hypoxia-mediated retinal neovascularization in mouse model of oxygen-induced retinopathy assessed as reduction in retinal neovascular tufts at 1 uM dosed via intravitreal route2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Novel Hypoxia-Inducible Factor 1α (HIF-1α) Inhibitors for Angiogenesis-Related Ocular Diseases: Discovery of a Novel Scaffold via Ring-Truncation Strategy.
AID1543583Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth at 1 uM after 72 hrs by MTT assay relative to control2019European journal of medicinal chemistry, Apr-01, Volume: 167Design, synthesis, and biological evaluation of truncated deguelin derivatives as Hsp90 inhibitors.
AID1543586Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Apr-01, Volume: 167Design, synthesis, and biological evaluation of truncated deguelin derivatives as Hsp90 inhibitors.
AID1255084Inhibition of STAT3 phosphorylation in human MCF10A cells transformed with H-ras at 10 uM after 24 hrs by Western blot analysis2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Identification of small molecule inhibitors of the STAT3 signaling pathway: Insights into their structural features and mode of action.
AID1543588Inhibition of FITC-geldanamycin binding to recombinant human full-length C-terminal His-tagged HSP90alpha N-terminal domain (1 to 732 residues) expressed in Escherichia coli after 1 hr by fluorescence polarization assay2019European journal of medicinal chemistry, Apr-01, Volume: 167Design, synthesis, and biological evaluation of truncated deguelin derivatives as Hsp90 inhibitors.
AID708843Inhibition of HSP90 in human H1299 cells assessed as reduction of HIF1alpha level treated for 72 hrs followed by incubated for 12 hrs under hypoxia condition by Western blot analysis2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Design, synthesis, and biological evaluation of novel deguelin-based heat shock protein 90 (HSP90) inhibitors targeting proliferation and angiogenesis.
AID1255082Inhibition of STAT3 transcriptional activity in human oncostatin M-stimulated HeLa cells at 10 uM after 24 hrs by luciferase reporter gene assay2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Identification of small molecule inhibitors of the STAT3 signaling pathway: Insights into their structural features and mode of action.
AID1604461Antiproliferative activity against human NCI-H1299 cells incubated for 2 days followed by medium replacement by MTT assay2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Heat Shock Protein 90 Inhibitors: An Update on Achievements, Challenges, and Future Directions.
AID1322390Inhibition of HSP90 in human H1299 cells assessed as suppression of HIF-1alpha at 100 nM preincubated for 72 hrs followed by incubation under hypoxic condition for 12 hrs by Western blot method relative to control2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Synthesis and biological evaluation of C-ring truncated deguelin derivatives as heat shock protein 90 (HSP90) inhibitors.
AID1543587Antiproliferative activity against human A549 cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Apr-01, Volume: 167Design, synthesis, and biological evaluation of truncated deguelin derivatives as Hsp90 inhibitors.
AID1543585Antiproliferative activity against human NCI-H1299 cells after 72 hrs by MTT assay2019European journal of medicinal chemistry, Apr-01, Volume: 167Design, synthesis, and biological evaluation of truncated deguelin derivatives as Hsp90 inhibitors.
AID1543582Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth at 0.1 uM after 72 hrs by MTT assay relative to control2019European journal of medicinal chemistry, Apr-01, Volume: 167Design, synthesis, and biological evaluation of truncated deguelin derivatives as Hsp90 inhibitors.
AID1387518Suppression of hypoxia-mediated retinal neovascularization in mouse model of oxygen-induced retinopathy assessed as reduction in retinal neovascular tufts at 100 nM dosed via intravitreal route2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Novel Hypoxia-Inducible Factor 1α (HIF-1α) Inhibitors for Angiogenesis-Related Ocular Diseases: Discovery of a Novel Scaffold via Ring-Truncation Strategy.
AID711217Antiangiogenic activity in transgenic zebrafish assessed as depletion of subintestinal veins after 72 hrs2012Journal of medicinal chemistry, Dec-27, Volume: 55, Issue:24
Design, synthesis, and biological evaluation of novel deguelin-based heat shock protein 90 (HSP90) inhibitors targeting proliferation and angiogenesis.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's8 (88.89)24.3611
2020's1 (11.11)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.21

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 Index12.21 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.21)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (11.11%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (88.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]