Compounds > 17-hydroxywortmannin
Page last updated: 2024-12-07

17-hydroxywortmannin

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

Description

## 17-Hydroxywortmannin: A Powerful Tool for Research

**17-Hydroxywortmannin** is a synthetic derivative of **wortmannin**, a natural product isolated from the fungus *Penicillium wortmanni*.

**Why is it important?**

17-Hydroxywortmannin acts as a **potent and selective inhibitor** of **phosphoinositide 3-kinase (PI3K)**, a family of enzymes playing crucial roles in various cellular processes, including:

* **Cell growth and proliferation:** PI3Ks regulate cell survival, growth, and division, making them important targets in cancer research.
* **Cell survival and apoptosis:** PI3Ks contribute to cell survival by inhibiting programmed cell death (apoptosis).
* **Metabolism:** PI3Ks impact glucose metabolism, insulin signaling, and lipid synthesis.
* **Immune response:** PI3Ks are involved in immune cell activation and differentiation.

**Significance in Research:**

17-Hydroxywortmannin's potent and selective inhibition of PI3Ks makes it a valuable tool for researchers studying various cellular processes and diseases. Specifically:

* **Cancer Research:** 17-Hydroxywortmannin is used to study the role of PI3Ks in cancer cell growth, survival, and metastasis. It may also hold potential as a therapeutic agent in cancer treatment.
* **Diabetes and Metabolic Disorders:** 17-Hydroxywortmannin helps researchers understand how PI3Ks affect insulin signaling and glucose metabolism. This knowledge could lead to better therapies for diabetes and other metabolic disorders.
* **Inflammation and Immunology:** 17-Hydroxywortmannin allows scientists to investigate the role of PI3Ks in immune cell activation and inflammation. This can contribute to the development of new immunotherapies and anti-inflammatory drugs.
* **Neurological Disorders:** PI3Ks are implicated in neurological disorders such as Alzheimer's disease and Parkinson's disease. 17-Hydroxywortmannin can be utilized to explore the role of PI3Ks in these conditions.

**Limitations:**

While 17-Hydroxywortmannin is a powerful tool, it is important to note that:

* **Off-target effects:** It can inhibit other kinases besides PI3Ks, limiting its specificity.
* **Pharmacokinetic limitations:** Its poor bioavailability and rapid metabolism pose challenges for in vivo studies.

**Conclusion:**

17-Hydroxywortmannin is a valuable research tool for exploring the diverse functions of PI3Ks in various cellular processes and disease pathways. It has the potential to contribute to the development of new therapeutic strategies for cancer, diabetes, inflammation, and other conditions. Further research and development are needed to overcome its limitations and fully exploit its potential.

17-hydroxywortmannin: inhibits secretion of human neutrophils [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9867340
CHEMBL ID273832
SCHEMBL ID8021215
MeSH IDM0151513

Synonyms (11)

Synonym
17beta-hydroxywortmannin
17-hydroxywortmannin
CHEMBL273832
SCHEMBL8021215
17-hydroxy-wortmannin
XLJORQYAOTYVQS-OGCOKEDGSA-N
17beta-hydroxy wortmannin
58053-83-1
[(1r,3r,5s,6s,9r,18s)-6-hydroxy-18-(methoxymethyl)-1,5-dimethyl-11,16-dioxo-13,17-dioxapentacyclo[10.6.1.02,10.05,9.015,19]nonadeca-2(10),12(19),14-trien-3-yl] acetate
17-hydroxy wortmannin
PD021155

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" Following a daily X5 dosing regimen, PWT-458 demonstrated single-agent antitumor activity in nude mouse xenograft models of U87MG glioma, nonsmall cell lung cancer (NSCLC) A549, and renal cell carcinoma (RCC) A498."( PWT-458, a novel pegylated-17-hydroxywortmannin, inhibits phosphatidylinositol 3-kinase signaling and suppresses growth of solid tumors.
Ayral-Kaloustian, S; Cai, P; Chaudhary, I; Fawzi, M; Frost, P; Gaydos, C; Gibbons, J; Gu, J; Li, F; Lotvin, J; Lucas, J; Mansour, T; Petersen, R; Ruppen, M; Skotnicki, J; Toral-Barza, L; Yu, K; Zask, A; Zhu, T, 2005)		0.33
[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)
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)IC50 (µMol)0.00270.00000.734010.0000AID320605
Serine/threonine-protein kinase mTORHomo sapiens (human)IC50 (µMol)0.19300.00000.857510.0000AID320606
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (131)

Processvia Protein(s)Taxonomy
phosphorylationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
angiogenesisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
liver developmentPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
regulation of protein phosphorylationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
vasculature developmentPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
glucose metabolic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phagocytosisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
epidermal growth factor receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
insulin receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of lamellipodium assemblyPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of gene expressionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to muscle inactivityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of macroautophagyPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
actin cytoskeleton organizationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
platelet activationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of actin filament depolymerizationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
T cell costimulationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of TOR signalingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cellular response to insulin stimulusPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to muscle stretchPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
vascular endothelial growth factor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
regulation of multicellular organism growthPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to L-leucinePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
anoikisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
regulation of cellular respirationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of neuron apoptotic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
endothelial cell migrationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol phosphate biosynthetic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
insulin-like growth factor receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of smooth muscle cell proliferationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
T cell receptor signaling pathwayPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
relaxation of cardiac musclePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cardiac muscle contractionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
adipose tissue developmentPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cellular response to glucose stimulusPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cellular response to hydrostatic pressurePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to dexamethasonePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cardiac muscle cell contractionPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
energy homeostasisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
regulation of actin filament organizationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
autosome genomic imprintingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
response to butyratePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
positive regulation of protein localization to membranePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of fibroblast apoptotic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
negative regulation of anoikisPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol-3-phosphate biosynthetic processPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol-mediated signalingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cell migrationPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
protein destabilizationSerine/threonine-protein kinase mTORHomo sapiens (human)
protein phosphorylationSerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of macroautophagySerine/threonine-protein kinase mTORHomo sapiens (human)
phosphorylationSerine/threonine-protein kinase mTORHomo sapiens (human)
protein autophosphorylationSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of cell growthSerine/threonine-protein kinase mTORHomo sapiens (human)
T-helper 1 cell lineage commitmentSerine/threonine-protein kinase mTORHomo sapiens (human)
heart morphogenesisSerine/threonine-protein kinase mTORHomo sapiens (human)
heart valve morphogenesisSerine/threonine-protein kinase mTORHomo sapiens (human)
energy reserve metabolic processSerine/threonine-protein kinase mTORHomo sapiens (human)
'de novo' pyrimidine nucleobase biosynthetic processSerine/threonine-protein kinase mTORHomo sapiens (human)
protein phosphorylationSerine/threonine-protein kinase mTORHomo sapiens (human)
inflammatory responseSerine/threonine-protein kinase mTORHomo sapiens (human)
DNA damage responseSerine/threonine-protein kinase mTORHomo sapiens (human)
cytoskeleton organizationSerine/threonine-protein kinase mTORHomo sapiens (human)
lysosome organizationSerine/threonine-protein kinase mTORHomo sapiens (human)
germ cell developmentSerine/threonine-protein kinase mTORHomo sapiens (human)
response to nutrientSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of cell sizeSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to starvationSerine/threonine-protein kinase mTORHomo sapiens (human)
response to heatSerine/threonine-protein kinase mTORHomo sapiens (human)
post-embryonic developmentSerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of autophagySerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of lamellipodium assemblySerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of gene expressionSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of epithelial to mesenchymal transitionSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of myotube differentiationSerine/threonine-protein kinase mTORHomo sapiens (human)
macroautophagySerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of macroautophagySerine/threonine-protein kinase mTORHomo sapiens (human)
phosphorylationSerine/threonine-protein kinase mTORHomo sapiens (human)
peptidyl-serine phosphorylationSerine/threonine-protein kinase mTORHomo sapiens (human)
neuronal action potentialSerine/threonine-protein kinase mTORHomo sapiens (human)
protein catabolic processSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of cell growthSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of actin filament polymerizationSerine/threonine-protein kinase mTORHomo sapiens (human)
T cell costimulationSerine/threonine-protein kinase mTORHomo sapiens (human)
ruffle organizationSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of myelinationSerine/threonine-protein kinase mTORHomo sapiens (human)
response to nutrient levelsSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to nutrient levelsSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to nutrientSerine/threonine-protein kinase mTORHomo sapiens (human)
TOR signalingSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of phosphoprotein phosphatase activitySerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to insulin stimulusSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of actin cytoskeleton organizationSerine/threonine-protein kinase mTORHomo sapiens (human)
calcineurin-NFAT signaling cascadeSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to amino acid starvationSerine/threonine-protein kinase mTORHomo sapiens (human)
multicellular organism growthSerine/threonine-protein kinase mTORHomo sapiens (human)
TORC1 signalingSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of circadian rhythmSerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of apoptotic processSerine/threonine-protein kinase mTORHomo sapiens (human)
response to amino acidSerine/threonine-protein kinase mTORHomo sapiens (human)
anoikisSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of osteoclast differentiationSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of translationSerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of cell sizeSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of glycolytic processSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIISerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of translational initiationSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of lipid biosynthetic processSerine/threonine-protein kinase mTORHomo sapiens (human)
behavioral response to painSerine/threonine-protein kinase mTORHomo sapiens (human)
rhythmic processSerine/threonine-protein kinase mTORHomo sapiens (human)
oligodendrocyte differentiationSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of oligodendrocyte differentiationSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationSerine/threonine-protein kinase mTORHomo sapiens (human)
voluntary musculoskeletal movementSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of stress fiber assemblySerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of keratinocyte migrationSerine/threonine-protein kinase mTORHomo sapiens (human)
nucleus localizationSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionSerine/threonine-protein kinase mTORHomo sapiens (human)
cardiac muscle cell developmentSerine/threonine-protein kinase mTORHomo sapiens (human)
cardiac muscle contractionSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to methionineSerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of calcineurin-NFAT signaling cascadeSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to amino acid stimulusSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to L-leucineSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to hypoxiaSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to osmotic stressSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of membrane permeabilitySerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of cellular response to heatSerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of protein localization to nucleusSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of signal transduction by p53 class mediatorSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of transcription of nucleolar large rRNA by RNA polymerase ISerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of wound healing, spreading of epidermal cellsSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of locomotor rhythmSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of cytoplasmic translational initiationSerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of lysosome organizationSerine/threonine-protein kinase mTORHomo sapiens (human)
positive regulation of pentose-phosphate shuntSerine/threonine-protein kinase mTORHomo sapiens (human)
cellular response to leucine starvationSerine/threonine-protein kinase mTORHomo sapiens (human)
regulation of autophagosome assemblySerine/threonine-protein kinase mTORHomo sapiens (human)
negative regulation of macroautophagySerine/threonine-protein kinase mTORHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (18)

Processvia Protein(s)Taxonomy
protein serine/threonine kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
protein bindingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
ATP bindingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
1-phosphatidylinositol-3-kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
protein kinase activator activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
insulin receptor substrate bindingPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
1-phosphatidylinositol-4,5-bisphosphate 3-kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
protein serine kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
1-phosphatidylinositol-4-phosphate 3-kinase activityPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
RNA polymerase III type 1 promoter sequence-specific DNA bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
RNA polymerase III type 2 promoter sequence-specific DNA bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
RNA polymerase III type 3 promoter sequence-specific DNA bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
TFIIIC-class transcription factor complex bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
protein kinase activitySerine/threonine-protein kinase mTORHomo sapiens (human)
protein serine/threonine kinase activitySerine/threonine-protein kinase mTORHomo sapiens (human)
protein bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
ATP bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
kinase activitySerine/threonine-protein kinase mTORHomo sapiens (human)
identical protein bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
ribosome bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
phosphoprotein bindingSerine/threonine-protein kinase mTORHomo sapiens (human)
protein serine kinase activitySerine/threonine-protein kinase mTORHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (24)

Processvia Protein(s)Taxonomy
cytosolPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol 3-kinase complex, class IAPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
intercalated discPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
lamellipodiumPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
perinuclear region of cytoplasmPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol 3-kinase complexPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
phosphatidylinositol 3-kinase complex, class IBPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
plasma membranePhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
cytoplasmPhosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformHomo sapiens (human)
PML bodySerine/threonine-protein kinase mTORHomo sapiens (human)
lysosomal membraneSerine/threonine-protein kinase mTORHomo sapiens (human)
cytosolSerine/threonine-protein kinase mTORHomo sapiens (human)
Golgi membraneSerine/threonine-protein kinase mTORHomo sapiens (human)
nucleoplasmSerine/threonine-protein kinase mTORHomo sapiens (human)
cytoplasmSerine/threonine-protein kinase mTORHomo sapiens (human)
mitochondrial outer membraneSerine/threonine-protein kinase mTORHomo sapiens (human)
lysosomeSerine/threonine-protein kinase mTORHomo sapiens (human)
lysosomal membraneSerine/threonine-protein kinase mTORHomo sapiens (human)
endoplasmic reticulum membraneSerine/threonine-protein kinase mTORHomo sapiens (human)
cytosolSerine/threonine-protein kinase mTORHomo sapiens (human)
endomembrane systemSerine/threonine-protein kinase mTORHomo sapiens (human)
membraneSerine/threonine-protein kinase mTORHomo sapiens (human)
dendriteSerine/threonine-protein kinase mTORHomo sapiens (human)
TORC1 complexSerine/threonine-protein kinase mTORHomo sapiens (human)
TORC2 complexSerine/threonine-protein kinase mTORHomo sapiens (human)
phagocytic vesicleSerine/threonine-protein kinase mTORHomo sapiens (human)
nuclear envelopeSerine/threonine-protein kinase mTORHomo sapiens (human)
nucleusSerine/threonine-protein kinase mTORHomo sapiens (human)
cytoplasmSerine/threonine-protein kinase mTORHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (9)

Assay IDTitleYearJournalArticle
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID320606Inhibition of mTOR2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy.
AID155514In vitro inhibitory activity against Phosphatidylinositol 3-Kinase1996Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5
Studies on the mechanism of phosphatidylinositol 3-kinase inhibition by wortmannin and related analogs.
AID134863In vivo inhibition of tumor growth in C3H Mammary model was evaluated at dose 1.0 mg/kg peroral administration1996Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5
Studies on the mechanism of phosphatidylinositol 3-kinase inhibition by wortmannin and related analogs.
AID320635Chemical stability at pH 7.42008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy.
AID134862In vivo inhibition of tumor growth in C3H Mammary model was evaluated at dose 0.50 mg/kg peroral administration1996Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5
Studies on the mechanism of phosphatidylinositol 3-kinase inhibition by wortmannin and related analogs.
AID320612Half life in mouse at 5 mg/kg, iv2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy.
AID320605Inhibition of PI3K expressed in Escherichia coli by microtiter plate-based fluorescence polarization assay2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy.
AID320613Growth inhibition of human LNCap cells2008Journal of medicinal chemistry, Mar-13, Volume: 51, Issue:5
Synthesis and structure-activity relationships of ring-opened 17-hydroxywortmannins: potent phosphoinositide 3-kinase inhibitors with improved properties and anticancer efficacy.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (15)

TimeframeStudies, This Drug (%)All Drugs %
pre-19903 (20.00)18.7374
1990's7 (46.67)18.2507
2000's4 (26.67)29.6817
2010's0 (0.00)24.3611
2020's1 (6.67)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other15 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one
2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one: specific inhibitor of phosphatidylinositol 3-kinase; structure in first source		1.9910chromones;
morpholines;
organochlorine compound		autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector
serine
Serine: A non-essential amino acid occurring in natural form as the L-isomer. It is synthesized from GLYCINE or THREONINE. It is involved in the biosynthesis of PURINES; PYRIMIDINES; and other amino acids.. serine : An alpha-amino acid that is alanine substituted at position 3 by a hydroxy group.		6.9710L-alpha-amino acid;
proteinogenic amino acid;
serine family amino acid;
serine zwitterion;
serine		algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
threonine
Threonine: An essential amino acid occurring naturally in the L-form, which is the active form. It is found in eggs, milk, gelatin, and other proteins.. threonine : An alpha-amino acid in which one of the hydrogens attached to the alpha-carbon of glycine is substituted by a 1-hydroxyethyl group.		6.9710amino acid zwitterion;
aspartate family amino acid;
L-alpha-amino acid;
proteinogenic amino acid;
threonine		algal metabolite;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
tetradecanoylphorbol acetate
Tetradecanoylphorbol Acetate: A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA.. phorbol ester : Esters of phorbol, originally found in croton oil (from Croton tiglium, of the family Euphorbiaceae). A number of phorbol esters possess activity as tumour promoters and activate the mechanisms associated with cell growth. Some of these are used in experiments as activators of protein kinase C.. phorbol 13-acetate 12-myristate : A phorbol ester that is phorbol in which the hydroxy groups at the cyclopropane ring juction (position 13) and the adjacent carbon (position 12) have been converted into the corresponding acetate and myristate esters. It is a major active constituent of the seed oil of Croton tiglium. It has been used as a tumour promoting agent for skin carcinogenesis in rodents and is associated with increased cell proliferation of malignant cells. However its function is controversial since a decrease in cell proliferation has also been observed in several cancer cell types.		2.3720acetate ester;
diester;
phorbol ester;
tertiary alpha-hydroxy ketone;
tetradecanoate ester		antineoplastic agent;
apoptosis inducer;
carcinogenic agent;
mitogen;
plant metabolite;
protein kinase C agonist;
reactive oxygen species generator
paclitaxel
Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).		2.0210taxane diterpenoid;
tetracyclic diterpenoid		antineoplastic agent;
human metabolite;
metabolite;
microtubule-stabilising agent
fura-2
Fura-2: A fluorescent calcium chelating agent which is used to study intracellular calcium in tissues.		1.9710
1-hexadecyl-2-acetyl-glycero-3-phosphocholine
Platelet Activating Factor: A phospholipid derivative formed by PLATELETS; BASOPHILS; NEUTROPHILS; MONOCYTES; and MACROPHAGES. It is a potent platelet aggregating agent and inducer of systemic anaphylactic symptoms, including HYPOTENSION; THROMBOCYTOPENIA; NEUTROPENIA; and BRONCHOCONSTRICTION.. 2-O-acetyl-1-O-hexadecyl-sn-glycero-3-phosphocholine : A 2-acetyl-1-alkyl-sn-glycero-3-phosphocholine betaine which has hexadecyl as the alkyl group. PAF is a potent phospholipid activator and mediator of many leukocyte functions, including platelet aggregation, inflammation, and anaphylaxis.		1.97102-acetyl-1-alkyl-sn-glycero-3-phosphocholineantihypertensive agent;
beta-adrenergic antagonist;
bronchoconstrictor agent;
hematologic agent;
vasodilator agent
benzofurans
Benzofurans: Compounds that contain a BENZENE ring fused to a furan ring.		1.9710
wortmannin
[no description available]		7.9140acetate ester;
cyclic ketone;
delta-lactone;
organic heteropentacyclic compound		anticoronaviral agent;
antineoplastic agent;
autophagy inhibitor;
EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor;
geroprotector;
Penicillium metabolite;
radiosensitizing agent
n-formylmethionine leucyl-phenylalanine
N-Formylmethionine Leucyl-Phenylalanine: A formylated tripeptide originally isolated from bacterial filtrates that is positively chemotactic to polymorphonuclear leucocytes, and causes them to release lysosomal enzymes and become metabolically activated.. N-formyl-L-methionyl-L-leucyl-L-phenylalanine : A tripeptide composed of L-Met, L-Leu and L-Phe in a linear sequence with a formyl group at the amino terminus. It acts as a potent inducer of leucocyte chemotaxis and macrophage activator as well as a ligand for the FPR receptor.		2.8940tripeptide
leukotriene b4
Leukotriene B4: The major metabolite in neutrophil polymorphonuclear leukocytes. It stimulates polymorphonuclear cell function (degranulation, formation of oxygen-centered free radicals, arachidonic acid release, and metabolism). (From Dictionary of Prostaglandins and Related Compounds, 1990). leukotriene B4 : A leukotriene composed of (6Z,8E,10E,14Z)-icosatetraenoic acid having (5S)- and (12R)-hydroxy substituents. It is a lipid mediator of inflammation that is generated from arachidonic acid via the 5-lipoxygenase pathway.		1.9710dihydroxy monocarboxylic acid;
hydroxy polyunsaturated fatty acid;
leukotriene;
long-chain fatty acid		human metabolite;
mouse metabolite;
plant metabolite;
vasoconstrictor agent
sirolimus
Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.. sirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent.		2.4320antibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol		antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
cytochalasin b
Cytochalasin B: A cytotoxic member of the CYTOCHALASINS.. cytochalasin B : An organic heterotricyclic compound, that is a mycotoxin which is cell permeable an an inhibitor of cytoplasmic division by blocking the formation of contractile microfilaments.		1.9810cytochalasin;
lactam;
lactone;
organic heterotricyclic compound		actin polymerisation inhibitor;
metabolite;
mycotoxin;
platelet aggregation inhibitor
staurosporine
staurosporinium : Conjugate acid of staurosporine.		1.9810ammonium ion derivative
px-866
PX-866: inhibitor of phosphoinositide-3-kinase signaling with antitumor activity; structure in first source. PX-866 : An organic heterotetracyclic compound that is obtained from wortmanin via aminolysis of its furan ring by diallyl amine.		2.0410acetate ester;
delta-lactone;
organic heterotetracyclic compound;
tertiary amino compound		EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor
phosphatidylcholines
Phosphatidylcholines: Derivatives of PHOSPHATIDIC ACIDS in which the phosphoric acid is bound in ester linkage to a CHOLINE moiety.		1.98101,2-diacyl-sn-glycero-3-phosphocholine
warfarin
Warfarin: An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.. warfarin : A racemate comprising equal amounts of (R)- and (S)-warfarin. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.. 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one : A member of the class of coumarins that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenyl-3-oxo-1-butyl group.		1.9810benzenes;
hydroxycoumarin;
methyl ketone
ConditionIndicatedRelationship StrengthStudiesTrials
Experimental Mammary Neoplasms
[description not available]		01.9910
Carcinoma, Non-Small Cell Lung
[description not available]		02.0210
Adenocarcinoma Of Kidney
[description not available]		02.0210
Glial Cell Tumors
[description not available]		02.4320
Cancer of Kidney
[description not available]		02.0210
Cancer of Lung
[description not available]		02.0210
Benign Neoplasms
[description not available]		02.0210
Carcinoma, Non-Small-Cell Lung
A heterogeneous aggregate of at least three distinct histological types of lung cancer, including SQUAMOUS CELL CARCINOMA; ADENOCARCINOMA; and LARGE CELL CARCINOMA. They are dealt with collectively because of their shared treatment strategy.		02.0210
Carcinoma, Renal Cell
A heterogeneous group of sporadic or hereditary carcinoma derived from cells of the KIDNEYS. There are several subtypes including the clear cells, the papillary, the chromophobe, the collecting duct, the spindle cells (sarcomatoid), or mixed cell-type carcinoma.		02.0210
Glioma
Benign and malignant central nervous system neoplasms derived from glial cells (i.e., astrocytes, oligodendrocytes, and ependymocytes). Astrocytes may give rise to astrocytomas (ASTROCYTOMA) or glioblastoma multiforme (see GLIOBLASTOMA). Oligodendrocytes give rise to oligodendrogliomas (OLIGODENDROGLIOMA) and ependymocytes may undergo transformation to become EPENDYMOMA; CHOROID PLEXUS NEOPLASMS; or colloid cysts of the third ventricle. (From Escourolle et al., Manual of Basic Neuropathology, 2nd ed, p21)		02.4320
Kidney Neoplasms
Tumors or cancers of the KIDNEY.		02.0210
Lung Neoplasms
Tumors or cancer of the LUNG.		02.0210
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		02.0210
Bone Loss, Osteoclastic
[description not available]		01.9910