Page last updated: 2024-11-12

hypothemycin

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Description

hypothemycin: a resorcylic acid lactone antibiotic; antifungal metabolite from Hypomyces trichothecoides [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

hypothemycin : A macrolide that is isolated from the cultured broth of Hypomyces subiculosus and shows antifungal activity and inhibits the growth of some human cancer cells. [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 CID9929643
CHEMBL ID471474
CHEBI ID83275
SCHEMBL ID10187414
MeSH IDM0332882

Synonyms (12)

Synonym
(1ar,8s,13s,14s,15ar)-5,13,14-trihydroxy-3-methoxy-8-methyl-8,9,13,14,15,15a-hexahydro-6h-oxireno[k][2]benzoxacyclotetradecine-6,12(1ah)-dione
hypothemycin
DB07905
CHEMBL471474
chebi:83275 ,
(1ar,8s,10z,13s,14s,15ar)-5,13,14-trihydroxy-3-methoxy-8-methyl-8,9,13,14,15,15a-hexahydro-6h-oxireno[k][2]benzoxacyclotetradecine-6,12(1ah)-dione
SCHEMBL10187414
bdbm50129131
AKOS027263555
hypothemycin, from hypomyces trichothecoides, >=98% (hplc)
Q27097139
DTXSID301017784

Research Excerpts

Overview

Hypothemycin is a macrolide protein kinase inhibitor from the fungus Hypomyces subiculosus.

ExcerptReferenceRelevance
"Hypothemycin is a macrolide protein kinase inhibitor from the fungus Hypomyces subiculosus. "( Enzymatic synthesis of resorcylic acid lactones by cooperation of fungal iterative polyketide synthases involved in hypothemycin biosynthesis.
Dorrestein, PC; Gao, Z; Li, JW; Meehan, MJ; Qiao, K; Tang, Y; Vederas, JC; Zhao, X; Zhou, H, 2010
)
2.01
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
EC 2.7.11.24 (mitogen-activated protein kinase) inhibitorAn EC 2.7.11.* (protein-serine/threonine kinase) inhibitor that interferes with the action of mitogen-activated protein kinase (EC 2.7.11.24).
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
fungal metaboliteAny eukaryotic metabolite produced during a metabolic reaction in fungi, the kingdom that includes microorganisms such as the yeasts and moulds.
antifungal agentAn antimicrobial agent that destroys fungi by suppressing their ability to grow or reproduce.
[role 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]

Drug Classes (8)

ClassDescription
macrolideA macrocyclic lactone with a ring of twelve or more members derived from a polyketide.
enoneAn alpha,beta-unsaturated ketone of general formula R(1)R(2)C=CR(3)-C(=O)R(4) (R(4) =/= H) in which the C=O function is conjugated to a C=C double bond at the alpha,beta position.
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
epoxideAny cyclic ether in which the oxygen atom forms part of a 3-membered ring.
diolA compound that contains two hydroxy groups, generally assumed to be, but not necessarily, alcoholic. Aliphatic diols are also called glycols.
polyketideNatural and synthetic compounds containing alternating carbonyl and methylene groups ('beta-polyketones'), biogenetically derived from repeated condensation of acetyl coenzyme A (via malonyl coenzyme A), and usually the compounds derived from them by further condensations, etc. Considered by many to be synonymous with the less frequently used terms acetogenins and ketides.
phenolsOrganic aromatic compounds having one or more hydroxy groups attached to a benzene or other arene ring.
secondary alpha-hydroxy ketoneAn alpha-hydroxy ketone in which the carbonyl group and the hydroxy group are linked by a carbon bearing one hydrogen and one organyl group. Secondary alpha-hydroxy ketones are also known as acyloins, and are formally derived from reductive coupling of two carboxylic acid groups.
[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 (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Mitogen-activated protein kinase kinase kinase 7Homo sapiens (human)IC50 (µMol)0.03300.00560.24702.6000AID1254043
Nuclear receptor subfamily 2 group C member 2Homo sapiens (human)IC50 (µMol)0.03000.00900.01950.0300AID1870096
Glycogen synthase kinase-3 betaHomo sapiens (human)IC50 (µMol)5.98150.00060.801310.0000AID1763943; AID1763944
TGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)IC50 (µMol)0.03000.00800.14710.9000AID1870096
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (129)

Processvia Protein(s)Taxonomy
MAPK cascadeMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
stimulatory C-type lectin receptor signaling pathwayMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
positive regulation of T cell cytokine productionMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
cytoplasmic pattern recognition receptor signaling pathwayMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
MyD88-dependent toll-like receptor signaling pathwayMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
chromatin remodelingMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
inflammatory responseMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
canonical NF-kappaB signal transductionMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
I-kappaB phosphorylationMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
JNK cascadeMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
negative regulation of gene expressionMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
positive regulation of macroautophagyMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
positive regulation of interleukin-2 productionMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
toll-like receptor 3 signaling pathwayMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
toll-like receptor 4 signaling pathwayMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
TRIF-dependent toll-like receptor signaling pathwayMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
nucleotide-binding domain, leucine rich repeat containing receptor signaling pathwayMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
p38MAPK cascadeMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
Fc-epsilon receptor signaling pathwayMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
interleukin-33-mediated signaling pathwayMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
interleukin-17A-mediated signaling pathwayMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
defense response to bacteriumMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
anoikisMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
positive regulation of JUN kinase activityMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
positive regulation of cell cycleMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
positive regulation of cell sizeMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
T cell receptor signaling pathwayMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
stress-activated MAPK cascadeMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
interleukin-1-mediated signaling pathwayMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
cellular response to tumor necrosis factorMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
cellular response to hypoxiaMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
cellular response to angiotensinMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell proliferationMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell migrationMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
immune responseMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor subfamily 2 group C member 2Homo sapiens (human)
regulation of DNA-templated transcriptionNuclear receptor subfamily 2 group C member 2Homo sapiens (human)
spermatogenesisNuclear receptor subfamily 2 group C member 2Homo sapiens (human)
nervous system developmentNuclear receptor subfamily 2 group C member 2Homo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor subfamily 2 group C member 2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IINuclear receptor subfamily 2 group C member 2Homo sapiens (human)
anatomical structure developmentNuclear receptor subfamily 2 group C member 2Homo sapiens (human)
cell differentiationNuclear receptor subfamily 2 group C member 2Homo sapiens (human)
positive regulation of embryonic developmentNuclear receptor subfamily 2 group C member 2Homo sapiens (human)
positive regulation of gene expressionGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of gene expressionGlycogen synthase kinase-3 betaHomo sapiens (human)
ER overload responseGlycogen synthase kinase-3 betaHomo sapiens (human)
peptidyl-serine phosphorylationGlycogen synthase kinase-3 betaHomo sapiens (human)
intracellular signal transductionGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of apoptotic processGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of protein export from nucleusGlycogen synthase kinase-3 betaHomo sapiens (human)
epithelial to mesenchymal transitionGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of cell-matrix adhesionGlycogen synthase kinase-3 betaHomo sapiens (human)
glycogen metabolic processGlycogen synthase kinase-3 betaHomo sapiens (human)
protein phosphorylationGlycogen synthase kinase-3 betaHomo sapiens (human)
mitochondrion organizationGlycogen synthase kinase-3 betaHomo sapiens (human)
dopamine receptor signaling pathwayGlycogen synthase kinase-3 betaHomo sapiens (human)
circadian rhythmGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of autophagyGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of gene expressionGlycogen synthase kinase-3 betaHomo sapiens (human)
peptidyl-serine phosphorylationGlycogen synthase kinase-3 betaHomo sapiens (human)
peptidyl-threonine phosphorylationGlycogen synthase kinase-3 betaHomo sapiens (human)
viral protein processingGlycogen synthase kinase-3 betaHomo sapiens (human)
hippocampus developmentGlycogen synthase kinase-3 betaHomo sapiens (human)
establishment of cell polarityGlycogen synthase kinase-3 betaHomo sapiens (human)
maintenance of cell polarityGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of cell migrationGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of axon extensionGlycogen synthase kinase-3 betaHomo sapiens (human)
neuron projection developmentGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of protein-containing complex assemblyGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of protein-containing complex assemblyGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of protein ubiquitinationGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of protein bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of proteasomal ubiquitin-dependent protein catabolic processGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of phosphoprotein phosphatase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of microtubule-based processGlycogen synthase kinase-3 betaHomo sapiens (human)
intracellular signal transductionGlycogen synthase kinase-3 betaHomo sapiens (human)
cellular response to interleukin-3Glycogen synthase kinase-3 betaHomo sapiens (human)
regulation of circadian rhythmGlycogen synthase kinase-3 betaHomo sapiens (human)
proteasome-mediated ubiquitin-dependent protein catabolic processGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of GTPase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of cell differentiationGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of osteoblast differentiationGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of glycogen biosynthetic processGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of cilium assemblyGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of protein catabolic processGlycogen synthase kinase-3 betaHomo sapiens (human)
protein autophosphorylationGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of protein export from nucleusGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of dendrite morphogenesisGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of axonogenesisGlycogen synthase kinase-3 betaHomo sapiens (human)
canonical Wnt signaling pathwayGlycogen synthase kinase-3 betaHomo sapiens (human)
excitatory postsynaptic potentialGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of microtubule cytoskeleton organizationGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of calcineurin-NFAT signaling cascadeGlycogen synthase kinase-3 betaHomo sapiens (human)
superior temporal gyrus developmentGlycogen synthase kinase-3 betaHomo sapiens (human)
cellular response to retinoic acidGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of canonical Wnt signaling pathwayGlycogen synthase kinase-3 betaHomo sapiens (human)
extrinsic apoptotic signaling pathwayGlycogen synthase kinase-3 betaHomo sapiens (human)
extrinsic apoptotic signaling pathway in absence of ligandGlycogen synthase kinase-3 betaHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionGlycogen synthase kinase-3 betaHomo sapiens (human)
neuron projection organizationGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of microtubule anchoring at centrosomeGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of cellular response to heatGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of protein localization to nucleusGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of long-term synaptic potentiationGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of mitochondrial outer membrane permeabilization involved in apoptotic signaling pathwayGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of protein acetylationGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of extrinsic apoptotic signaling pathway via death domain receptorsGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of protein localization to ciliumGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of dopaminergic neuron differentiationGlycogen synthase kinase-3 betaHomo sapiens (human)
cellular response to amyloid-betaGlycogen synthase kinase-3 betaHomo sapiens (human)
positive regulation of protein localization to centrosomeGlycogen synthase kinase-3 betaHomo sapiens (human)
beta-catenin destruction complex disassemblyGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of type B pancreatic cell developmentGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of glycogen (starch) synthase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of mesenchymal stem cell differentiationGlycogen synthase kinase-3 betaHomo sapiens (human)
negative regulation of TOR signalingGlycogen synthase kinase-3 betaHomo sapiens (human)
regulation of neuron projection developmentGlycogen synthase kinase-3 betaHomo sapiens (human)
cell differentiationGlycogen synthase kinase-3 betaHomo sapiens (human)
insulin receptor signaling pathwayGlycogen synthase kinase-3 betaHomo sapiens (human)
in utero embryonic developmentTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
heart morphogenesisTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
cardiac septum developmentTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
lung developmentTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
aorta developmentTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
non-canonical NF-kappaB signal transductionTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
positive regulation of MAPK cascadeTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
coronary vasculature developmentTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
positive regulation of protein serine/threonine kinase activityTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
positive regulation of cGAS/STING signaling pathwayTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
protein dephosphorylationTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (44)

Processvia Protein(s)Taxonomy
magnesium ion bindingMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
transcription coactivator bindingMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
protein serine/threonine kinase activityMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
MAP kinase activityMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
MAP kinase kinase kinase activityMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
type II transforming growth factor beta receptor bindingMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
protein bindingMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
ATP bindingMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
MAP kinase kinase kinase kinase activityMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
receptor tyrosine kinase bindingMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
ubiquitin protein ligase bindingMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
histone kinase activityMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
identical protein bindingMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
scaffold protein bindingMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
protein serine kinase activityMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
protein serine/threonine kinase bindingMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
DNA-binding transcription factor bindingMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
linear polyubiquitin bindingMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingNuclear receptor subfamily 2 group C member 2Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor subfamily 2 group C member 2Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor subfamily 2 group C member 2Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificNuclear receptor subfamily 2 group C member 2Homo sapiens (human)
DNA-binding transcription factor activityNuclear receptor subfamily 2 group C member 2Homo sapiens (human)
protein bindingNuclear receptor subfamily 2 group C member 2Homo sapiens (human)
zinc ion bindingNuclear receptor subfamily 2 group C member 2Homo sapiens (human)
sequence-specific DNA bindingNuclear receptor subfamily 2 group C member 2Homo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor subfamily 2 group C member 2Homo sapiens (human)
nuclear receptor activityNuclear receptor subfamily 2 group C member 2Homo sapiens (human)
protease bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
p53 bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
protein kinase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
protein serine/threonine kinase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
protein bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
ATP bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
beta-catenin bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
kinase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
protein kinase bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
ubiquitin protein ligase bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
protein kinase A catalytic subunit bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
dynactin bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
tau protein bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
tau-protein kinase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
NF-kappaB bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingGlycogen synthase kinase-3 betaHomo sapiens (human)
protein serine kinase activityGlycogen synthase kinase-3 betaHomo sapiens (human)
protein serine/threonine phosphatase activityTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
protein bindingTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
protein serine/threonine kinase activator activityTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
protein-containing complex bindingTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
mitogen-activated protein kinase p38 bindingTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
molecular adaptor activityTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (21)

Processvia Protein(s)Taxonomy
cytoplasmMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
cytosolMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
nucleusMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
cytosolMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
plasma membraneMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
endosome membraneMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
ATAC complexMitogen-activated protein kinase kinase kinase 7Homo sapiens (human)
nucleoplasmNuclear receptor subfamily 2 group C member 2Homo sapiens (human)
chromatinNuclear receptor subfamily 2 group C member 2Homo sapiens (human)
glutamatergic synapseGlycogen synthase kinase-3 betaHomo sapiens (human)
nucleusGlycogen synthase kinase-3 betaHomo sapiens (human)
nucleoplasmGlycogen synthase kinase-3 betaHomo sapiens (human)
cytoplasmGlycogen synthase kinase-3 betaHomo sapiens (human)
mitochondrionGlycogen synthase kinase-3 betaHomo sapiens (human)
centrosomeGlycogen synthase kinase-3 betaHomo sapiens (human)
cytosolGlycogen synthase kinase-3 betaHomo sapiens (human)
plasma membraneGlycogen synthase kinase-3 betaHomo sapiens (human)
axonGlycogen synthase kinase-3 betaHomo sapiens (human)
dendriteGlycogen synthase kinase-3 betaHomo sapiens (human)
beta-catenin destruction complexGlycogen synthase kinase-3 betaHomo sapiens (human)
presynapseGlycogen synthase kinase-3 betaHomo sapiens (human)
postsynapseGlycogen synthase kinase-3 betaHomo sapiens (human)
Wnt signalosomeGlycogen synthase kinase-3 betaHomo sapiens (human)
cytosolGlycogen synthase kinase-3 betaHomo sapiens (human)
axonGlycogen synthase kinase-3 betaHomo sapiens (human)
nucleusGlycogen synthase kinase-3 betaHomo sapiens (human)
cytoplasmGlycogen synthase kinase-3 betaHomo sapiens (human)
cytoplasmTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
endoplasmic reticulumTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
endoplasmic reticulum membraneTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
cytosolTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
endosome membraneTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
nuclear speckTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
protein-containing complexTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
cytosolTGF-beta-activated kinase 1 and MAP3K7-binding protein 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (38)

Assay IDTitleYearJournalArticle
AID379156Cytotoxicity against human HT-29 cells2006Journal of natural products, Oct, Volume: 69, Issue:10
Cytotoxic hypothemycin analogues from Hypomyces subiculosus.
AID1870096Inhibition of recombinant human N-terminal GST-tagged TAK1 (1 to 303 residues)/TAB1 (437 to end residues) expressed in baculovirus infected Sf9 insect cells using myelin basic protein as substrate preincubated for 10 mins followed by ATP addition and meas2022Journal of natural products, 08-26, Volume: 85, Issue:8
Semisynthesis of Hypothemycin Analogues Targeting the C8-C9 Diol.
AID1763944Inhibition of human GSK-3beta preincubated for 3 hrs followed by ATP and substrate addition measured by serial dilution assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40A novel GSK-3 inhibitor binds to GSK-3β via a reversible, time and Cys-199-dependent mechanism.
AID379154Cytotoxicity against human SKOV3 cells2006Journal of natural products, Oct, Volume: 69, Issue:10
Cytotoxic hypothemycin analogues from Hypomyces subiculosus.
AID1602315Toxicity in zebrafish embryo assessed as mortality at 10 uM measured 120 hpf by fluorescence microscopy2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations.
AID1378627Cytotoxicity against human HeLa cells after 72 hrs by MTT assay2017Journal of natural products, 08-25, Volume: 80, Issue:8
Antifungal and Cytotoxic β-Resorcylic Acid Lactones from a Paecilomyces Species.
AID1602304Cytotoxicity in human THP1 cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations.
AID1602362Inhibition of covalent binding of 50 uM (Z)-N-(2-(2-(4-(2,8-Diethyl-5,5-difluoro-1,3,7,9-tetramethyl-5H-4lambda4,5lambda4-dipyrrolo[1,2-c:2',1'-f ][1,3,2]diazaborinin-10-yl)phenoxy)-acetamido)ethyl)-2,4-dimethyl-5-((2-oxo-5-(vinylsulfon-amido)-indolin-3-y2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations.
AID1378629Antifungal activity against Fusarium verticillioides after 8 hrs by conidial germination assay2017Journal of natural products, 08-25, Volume: 80, Issue:8
Antifungal and Cytotoxic β-Resorcylic Acid Lactones from a Paecilomyces Species.
AID1870098Cytotoxicity against human MDA-MB-435 cells assessed as reduction in cell viability measured after 72 hrs by celltiter-blue cell viability assay2022Journal of natural products, 08-26, Volume: 85, Issue:8
Semisynthesis of Hypothemycin Analogues Targeting the C8-C9 Diol.
AID1602301Irreversible inhibition of recombinant human FLT3 D835Y mutant (571 to 993 residues) expressed in baculovirus expression system at 1 uM preincubated for 5 to 30 mins followed by myelobasic protein addition and measured after 120 mins in presence of ATP by2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations.
AID379155Cytotoxicity against human COLO829 cells2006Journal of natural products, Oct, Volume: 69, Issue:10
Cytotoxic hypothemycin analogues from Hypomyces subiculosus.
AID1763935Reversible inhibition of recombinant human GSK-3beta at 20 uM preincubated for 3 hrs followed by diluted with substrate and ATP master mix solution measured upto 1.5 hrs by jump dilution assays2021Bioorganic & medicinal chemistry, 06-15, Volume: 40A novel GSK-3 inhibitor binds to GSK-3β via a reversible, time and Cys-199-dependent mechanism.
AID1763942Reversible inhibition of recombinant human GSK-3beta at 100 nM incubated with substrate and ATP master mix solution by jump dilution assays2021Bioorganic & medicinal chemistry, 06-15, Volume: 40A novel GSK-3 inhibitor binds to GSK-3β via a reversible, time and Cys-199-dependent mechanism.
AID1254043Inhibition of TAK1 (unknown origin)2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Isolation, semisynthesis, covalent docking and transforming growth factor beta-activated kinase 1 (TAK1)-inhibitory activities of (5Z)-7-oxozeaenol analogues.
AID1763943Inhibition of human GSK-3beta incubated with substrate in presence of ATP measured by serial dilution assay2021Bioorganic & medicinal chemistry, 06-15, Volume: 40A novel GSK-3 inhibitor binds to GSK-3β via a reversible, time and Cys-199-dependent mechanism.
AID606022Cytotoxicity against human MCF7 cells after 72 hrs by MTS assay2011Journal of natural products, May-27, Volume: 74, Issue:5
Resorcylic acid lactones with cytotoxic and NF-κB inhibitory activities and their structure-activity relationships.
AID606023Cytotoxicity against human H460 cells after 72 hrs by MTS assay2011Journal of natural products, May-27, Volume: 74, Issue:5
Resorcylic acid lactones with cytotoxic and NF-κB inhibitory activities and their structure-activity relationships.
AID1763934Reversible inhibition of recombinant human GSK-3beta at 70 uM preincubated for 3 hrs followed by diluted with substrate and ATP master mix solution measured upto 1.5 hrs by jump dilution assays2021Bioorganic & medicinal chemistry, 06-15, Volume: 40A novel GSK-3 inhibitor binds to GSK-3β via a reversible, time and Cys-199-dependent mechanism.
AID1602298Cytotoxicity in human MV4-11 cells assessed as inhibition of cellular viability incubated for 72 hrs by CellTiter-Blue assay2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations.
AID606024Cytotoxicity against human SF268 cells after 72 hrs by MTS assay2011Journal of natural products, May-27, Volume: 74, Issue:5
Resorcylic acid lactones with cytotoxic and NF-κB inhibitory activities and their structure-activity relationships.
AID1602303Irreversible inhibition of recombinant human FLT3 ITD mutant (571 to 993 residues) expressed in baculovirus expression system at 0.1 uM preincubated for 5 to 30 mins followed by myelobasic protein addition measured after 120 mins in presence of ATP by ADP2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations.
AID1763947Inhibition of human GSK-3beta at 10 uM in presence of 2 mM GSH by kinase-profiling analysis2021Bioorganic & medicinal chemistry, 06-15, Volume: 40A novel GSK-3 inhibitor binds to GSK-3β via a reversible, time and Cys-199-dependent mechanism.
AID606025Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTS assay2011Journal of natural products, May-27, Volume: 74, Issue:5
Resorcylic acid lactones with cytotoxic and NF-κB inhibitory activities and their structure-activity relationships.
AID1378625Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay2017Journal of natural products, 08-25, Volume: 80, Issue:8
Antifungal and Cytotoxic β-Resorcylic Acid Lactones from a Paecilomyces Species.
AID1602302Irreversible inhibition of recombinant human FLT3 D835Y mutant (571 to 993 residues) expressed in baculovirus expression system at 0.1 uM preincubated for 5 to 30 mins followed by myelobasic protein addition measured after 120 mins in presence of ATP by A2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations.
AID1602305Cytotoxicity in human Jurkat cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations.
AID1763941Reversible inhibition of recombinant human GSK-3beta at 200 nM incubated with substrate and ATP master mix solution by jump dilution assays2021Bioorganic & medicinal chemistry, 06-15, Volume: 40A novel GSK-3 inhibitor binds to GSK-3β via a reversible, time and Cys-199-dependent mechanism.
AID1763946Inhibition of human GSK-3beta at 10 uM in presence of 2 mM TCEP by kinase-profiling analysis2021Bioorganic & medicinal chemistry, 06-15, Volume: 40A novel GSK-3 inhibitor binds to GSK-3β via a reversible, time and Cys-199-dependent mechanism.
AID1602306Half life of the compound in potassium phosphate buffer at 10 uM in presence of 100 fold excess reduced glutathione by HPLC analysis2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations.
AID606021Cytotoxicity against human HT-29 cells after 72 hrs by MTS assay2011Journal of natural products, May-27, Volume: 74, Issue:5
Resorcylic acid lactones with cytotoxic and NF-κB inhibitory activities and their structure-activity relationships.
AID1378628Antifungal activity against Peronophythora litchii after 8 hrs by conidial germination assay2017Journal of natural products, 08-25, Volume: 80, Issue:8
Antifungal and Cytotoxic β-Resorcylic Acid Lactones from a Paecilomyces Species.
AID652589Inhibition of MAP2011ACS medicinal chemistry letters, Sep-08, Volume: 2, Issue:9
Exploring aigialomycin d and its analogues as protein kinase inhibitors for cancer targets.
AID1763945Inhibition of human GSK-3beta at 10 uM in presence of 2 mM DTT by kinase-profiling analysis2021Bioorganic & medicinal chemistry, 06-15, Volume: 40A novel GSK-3 inhibitor binds to GSK-3β via a reversible, time and Cys-199-dependent mechanism.
AID1763940Reversible inhibition of recombinant human GSK-3beta at 700 nM incubated with substrate and ATP master mix solution by jump dilution assays2021Bioorganic & medicinal chemistry, 06-15, Volume: 40A novel GSK-3 inhibitor binds to GSK-3β via a reversible, time and Cys-199-dependent mechanism.
AID1378626Cytotoxicity against human A549 cells after 72 hrs by MTT assay2017Journal of natural products, 08-25, Volume: 80, Issue:8
Antifungal and Cytotoxic β-Resorcylic Acid Lactones from a Paecilomyces Species.
AID1870097Cytotoxicity against human OVCAR-3 cells assessed as reduction in cell viability measured after 72 hrs by celltiter-blue cell viability assay2022Journal of natural products, 08-26, Volume: 85, Issue:8
Semisynthesis of Hypothemycin Analogues Targeting the C8-C9 Diol.
AID1602321Binding affinity to wild type FLT3 (unknown origin) assessed as covalent modification at Cys828 residue by MALDI-TOF spectrometric analysis2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Virtual Screening Identifies Irreversible FMS-like Tyrosine Kinase 3 Inhibitors with Activity toward Resistance-Conferring Mutations.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (35)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's4 (11.43)18.2507
2000's11 (31.43)29.6817
2010's16 (45.71)24.3611
2020's4 (11.43)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 22.97

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index22.97 (24.57)
Research Supply Index3.58 (2.92)
Research Growth Index4.91 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (22.97)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (8.57%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other32 (91.43%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]