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celastrol
(9b,13a,14b,20a)-3-hydroxy-9,13-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oic acid

Supplier Sponsors

Name:(2R,4aS,6aR,6aS,14aS,14bR)-10-hydroxy-2,4a,6a,6a,9,14a-hexamethyl-11-oxo-1,3,4,5,6,13,14,14b-octahydropicene-2-carboxylic acid
CAS Number: 34157-83-0Picture of molecule3D/inchi
FDA UNII: L8GG98663L
Nikkaji Web:J18.706B
MDL:MFCD03424073
XlogP3-AA:5.90 (est)
Molecular Weight:450.61866000
Formula:C29 H38 O4
BioActivity Summary:listing
NMR Predictor:Predict (works with chrome, Edge or firefox)
Category:natural substances and extractives
 
US / EU / FDA / JECFA / FEMA / FLAVIS / Scholar / Patent Information:
Google Scholar:Search
Google Books:Search
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Google Scholar: with word "flavor"Search
Google Scholar: with word "odor"Search
Google Patents:Search
US Patents:Search
EU Patents:Search
Pubchem Patents:Search
PubMed:Search
NCBI:Search
 
Physical Properties:
Assay: 95.00 to 100.00
Food Chemicals Codex Listed: No
Boiling Point: 645.70 °C. @ 760.00 mm Hg (est)
Flash Point: 677.00 °F. TCC ( 358.30 °C. ) (est)
logP (o/w): 7.080 (est)
Soluble in:
 water, 0.02106 mg/L @ 25 °C (est)
 
Organoleptic Properties:
Odor and/or flavor descriptions from others (if found).
 
Cosmetic Information:
None found
 
Suppliers:
Alfa Biotechnology
For experimental / research use only.
Celastrol 98%
BOC Sciences
For experimental / research use only.
Celastrol >98%
Odor: characteristic
Use: Celastrol (tripterine) is a chemical compound isolated from the root extracts of Tripterygium wilfordii (Thunder god vine) and Celastrus regelii. Celastrol is a pentacyclic triterpenoid and belongs to the family of quinone methides.
Carbosynth
For experimental / research use only.
Celastrol
Coompo
For experimental / research use only.
Celastrol from Plants ≥98%
Odor: characteristic
Use: Celastrol is a triterpenoid antioxidant compound isolated from the Chinese Thunder of God vine (Tripterygium wilfordii Hook. f.). In an isolated rat liver assay of lipid peroxidation, celastrol had an IC50 value of 7 µM, equivalent to about 15 times the antioxidant potency of a-tocopherol. An antioxidant natural product which inhibits the growth of human glioma xenografts in nude mice through suppressing VEGFR expression. Used for clinical treatment for rheumatoid arthritis, was demonstrated to have antiangiogenic activity, and be inhibitory against mice tumor growth by a few recent studies.
Glentham Life Sciences
Celastrol
Santa Cruz Biotechnology
For experimental / research use only.
Celastrol, Celastrus scandens ≥98%
Sigma-Aldrich: Sigma
For experimental / research use only.
Celastrol ≥98% (HPLC), solid
sds
Tocris Bioscience
For experimental / research use only.
Celastrol >99 %
 
Safety Information:
Preferred SDS: View
 
Hazards identification
 
Classification of the substance or mixture
GHS Classification in accordance with 29 CFR 1910 (OSHA HCS)
None found.
GHS Label elements, including precautionary statements
 
Pictogram
 
Hazard statement(s)
None found.
Precautionary statement(s)
None found.
Oral/Parenteral Toxicity:
Not determined
Dermal Toxicity:
Not determined
Inhalation Toxicity:
Not determined
 
Safety in Use Information:
Category:
natural substances and extractives
Recommendation for celastrol usage levels up to:
 not for fragrance use.
 
Recommendation for celastrol flavor usage levels up to:
 not for flavor use.
 
Safety References:
EPI System: View
AIDS Citations:Search
Cancer Citations:Search
Toxicology Citations:Search
EPA ACToR:Toxicology Data
EPA Substance Registry Services (SRS):Registry
Laboratory Chemical Safety Summary :122724
National Institute of Allergy and Infectious Diseases:Data
WGK Germany:2
(2R,4aS,6aR,6aS,14aS,14bR)-10-hydroxy-2,4a,6a,6a,9,14a-hexamethyl-11-oxo-1,3,4,5,6,13,14,14b-octahydropicene-2-carboxylic acid
Chemidplus:0034157830
 
References:
 (2R,4aS,6aR,6aS,14aS,14bR)-10-hydroxy-2,4a,6a,6a,9,14a-hexamethyl-11-oxo-1,3,4,5,6,13,14,14b-octahydropicene-2-carboxylic acid
NIST Chemistry WebBook:Search Inchi
Pubchem (cid):122724
Pubchem (sid):135079953
 
Other Information:
(IUPAC):Atomic Weights of the Elements 2011 (pdf)
Videos:The Periodic Table of Videos
tgsc:Atomic Weights use for this web site
(IUPAC):Periodic Table of the Elements
CHEBI:View
CHEMBL:View
HMDB (The Human Metabolome Database):HMDB02385
FooDB:FDB022989
VCF-Online:VCF Volatile Compounds in Food
ChemSpider:View
Wikipedia:View
 
Potential Blenders and core components note
None Found
 
Potential Uses:
None Found
 
Occurrence (nature, food, other):note
 found in nature
 
Synonyms:
(2R,4aS,6aS,12bR,14aS,14bR)-10-Hydroxy-2,4a,6a,9,12b,14a-hexamethyl-11-oxo-1,2,3,4,4a,5,6,6a,11,12b,13,14,14a,14b-tetradecahydro-picene-2-carboxylic acid
(20a)-3-hydroxy-2-oxo-D:A-Friedo-24-noroleana-1(10),3,5,7-tetraen-29-oic acid
(2R,4aS,6aR,6aS,14aS,14bR)-10-hydroxy-2,4a,6a,6a,9,14a-hexamethyl-11-oxo-1,3,4,5,6,13,14,14b-octahydropicene-2-carboxylic acid
(2R,4aS,6aS,12bR,14aS,14bR)-10-hydroxy-2,4a,6a,9,12b,14a-hexamethyl-11-oxo-1,2,3,4,4a,5,6,6a,11,12b,13,14,14a,14b-tetradecahydro-2-picenecarboxylic acid
(2R,4aS,6aS,12bR,14aS,14bR)-10-hydroxy-2,4a,6a,9,12b,14a-hexamethyl-11-oxo-1,3,4,5,6,13,14,14b-octahydropicene-2-carboxylic acid
3-hydroxy-24-nor-2-oxo-1(10),3,5,7-friedelatetraen-29-oic acid
(9b,13a,14b,20a)-3-hydroxy-9,13-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oic acid
2-picenecarboxylic acid, 1,2,3,4,4a,5,6,6a, 11,12b,13,14,14a,14b-tetradecahydro-10-hydroxy-2,4a,6a,9,12b, 14a-hexamethyl-11-oxo-
2-picenecarboxylic acid, 1,2,3,4,4a,5,6,6a,11,12b,13,14,14a,14b-tetradecahydro-10-hydroxy-2,4a,6a,9,12b,14a-hexamethyl-11-oxo-, (2R,4aS,6aS,12bR,14aS,14bR)-
(2R,4aS,6aS,12bR,14aS,14bR)-1,2,3,4,4a,5,6,6a,11,12b,13,14,14a,14b-tetradecahydro-10-hydroxy-2,4a,6a,9,12b,14a-hexamethyl-11-oxo-2-picenecarboxylic acid
1,2,3,4,4a,5,6,6a, 11,12b,13,14,14a,14b-tetradecahydro-10-hydroxy-2,4a,6a,9,12b,14a-hexamethyl-11-oxo-2-picenecarboxylic acid
 tripterin
 tripterine
 

Articles:

PubMed:Decrease of CD68 Synovial Macrophages in Celastrol Treated Arthritic Rats.
PubMed:Caloric restriction and exercise "mimetics'': Ready for prime time?
PubMed:Targeting acute myeloid leukemia with a small molecule inhibitor of the Myb/p300 interaction.
PubMed:Nanoencapsulation of natural triterpenoid celastrol for prostate cancer treatment.
PubMed:Inhibiting inducible miR-223 further reduces viable cells in human cancer cell lines MCF-7 and PC3 treated by celastrol.
PubMed:Targeting Mast Cells and Basophils with Anti-FcεRIα Fab-Conjugated Celastrol-Loaded Micelles Suppresses Allergic Inflammation.
PubMed:Celastrol induces cell cycle arrest by MicroRNA-21-mTOR-mediated inhibition p27 protein degradation in gastric cancer.
PubMed:Direct inhibition of c-Myc-Max heterodimers by celastrol and celastrol-inspired triterpenoids.
PubMed:Celastrol Induces Autophagy by Targeting AR/miR-101 in Prostate Cancer Cells.
PubMed:The natural compound celastrol inhibits necroptosis and alleviates ulcerative colitis in mice.
PubMed:Synergistic anticancer effects of triptolide and celastrol, two main compounds from thunder god vine.
PubMed:Disruption of Heat Shock Protein 90 (Hsp90)-Protein Kinase Cδ (PKCδ) Interaction by (-)-Maackiain Suppresses Histamine H1 Receptor Gene Transcription in HeLa Cells.
PubMed:Simultaneous determination of triptolide, tripterifordin, celastrol and nine sesquiterpene alkaloids in Tripterygium preparations using high-performance liquid chromatography-triple quadrupole mass spectrometry.
PubMed:Celastrol Protects against Obesity and Metabolic Dysfunction through Activation of a HSF1-PGC1α Transcriptional Axis.
PubMed:Total Synthesis of Celastrol, Development of a Platform to Access Celastroid Natural Products.
PubMed:Expression profile of heat shock response factors during hookworm larval activation and parasitic development.
PubMed:Cloning and functional characterization of an isopentenyl diphosphate isomerase gene from Tripterygium wilfordii.
PubMed:Hsp90 Activity Modulation by Plant Secondary Metabolites.
PubMed:[Effect of celastrol in inhibiting metastasis of lung cancer cells by influencing Akt signaling pathway and expressing integrins].
PubMed:Sugar-decorated mesoporous silica nanoparticles as delivery vehicles for the poorly soluble drug celastrol enables targeted induction of apoptosis in cancer cells.
PubMed:Celastrol induces apoptosis of human osteosarcoma cells via the mitochondrial apoptotic pathway.
PubMed:Tubulin Beta3 Serves as a Target of HDAC3 and Mediates Resistance to Microtubule-Targeting Drugs.
PubMed:Inhibition of inflammation with celastrol fails to improve muscle function in dysferlin-deficient A/J mice.
PubMed:Celastrol blocks binding of lipopolysaccharides to a Toll-like receptor4/myeloid differentiation factor2 complex in a thiol-dependent manner.
PubMed:[Anti-metastasis of celastrol on esophageal cancer cells and its mechanism].
PubMed:Celastrol identified as a leptin sensitizer and potential novel treatment for obesity.
PubMed:Treatment of obesity with celastrol.
PubMed:Withaferin A Regulates LRRK2 Levels by Interfering with the Hsp90- Cdc37 Chaperone Complex.
PubMed:Celastrol Protects against Antimycin A-Induced Insulin Resistance in Human Skeletal Muscle Cells.
PubMed:Celastrol inhibits inflammatory stimuli-induced neutrophil extracellular trap formation.
PubMed:Celastrol overcomes HSP72 gene silencing-mediated muscle atrophy and induces myofiber preservation.
PubMed:Celastrol induces proteasomal degradation of FANCD2 to sensitize lung cancer cells to DNA crosslinking agents.
PubMed:Effect of celastrol on growth inhibition of prostate cancer cells through the regulation of hERG channel in vitro.
PubMed:Celastrol ameliorates experimental colitis in IL-10 deficient mice via the up-regulation of autophagy.
PubMed:Anticancer effect of celastrol on human triple negative breast cancer: possible involvement of oxidative stress, mitochondrial dysfunction, apoptosis and PI3K/Akt pathways.
PubMed:Celastrol supports survival of retinal ganglion cells injured by optic nerve crush.
PubMed:Design and synthesis of celastrol derivatives as anticancer agents.
PubMed:Inhibitory mechanisms of celastrol on human liver cytochrome P450 1A2, 2C19, 2D6, 2E1 and 3A4.
PubMed:Effects of Plants and Isolates of Celastraceae Family on Cancer Pathways.
PubMed:Effects of natural nuclear factor-kappa B inhibitors on anticancer drug efflux transporter human P-glycoprotein.
PubMed:Celastrol Ameliorates EAE Induction by Suppressing Pathogenic T Cell Responses in the Peripheral and Central Nervous Systems.
PubMed:Celastrol, a Chinese herbal compound, controls autoimmune inflammation by altering the balance of pathogenic and regulatory T cells in the target organ.
PubMed:Celastrol induces mitochondria-mediated apoptosis in hepatocellular carcinoma Bel-7402 cells.
PubMed:Celastrol induces apoptosis and autophagy via the ROS/JNK signaling pathway in human osteosarcoma cells: an in vitro and in vivo study.
PubMed:Celastrol prevents circulatory failure via induction of heme oxygenase-1 and heat shock protein 70 in endotoxemic rats.
PubMed:Celastrol attenuates bone erosion in collagen-Induced arthritis mice and inhibits osteoclast differentiation and function in RANKL-induced RAW264.7.
PubMed:Amelioration of mitochondrial dysfunction-induced insulin resistance in differentiated 3T3-L1 adipocytes via inhibition of NF-κB pathways.
PubMed:Tumor necrosis factor-α sensitizes breast cancer cells to natural products with proteasome-inhibitory activity leading to apoptosis.
PubMed:Celastrol stimulates hypoxia-inducible factor-1 activity in tumor cells by initiating the ROS/Akt/p70S6K signaling pathway and enhancing hypoxia-inducible factor-1α protein synthesis.
PubMed:Redox-active compounds with a history of human use: antistaphylococcal action and potential for repurposing as topical antibiofilm agents.
PubMed:ATF2 contributes to cisplatin resistance in non-small cell lung cancer and celastrol induces cisplatin resensitization through inhibition of JNK/ATF2 pathway.
PubMed:Heat-induced expression of the immediate-early gene IER5 and its involvement in the proliferation of heat-shocked cells.
PubMed:Celastrol induces the apoptosis of breast cancer cells and inhibits their invasion via downregulation of MMP-9.
PubMed:Celastrol suppresses obesity process via increasing antioxidant capacity and improving lipid metabolism.
PubMed:Celastrol, an oral heat shock activator, ameliorates multiple animal disease models of cell death.
PubMed:Celastrol inhibits Plasmodium falciparum enoyl-acyl carrier protein reductase.
PubMed:Characterization of eight terpenoids from tissue cultures of the Chinese herbal plant, Tripterygium wilfordii, by high-performance liquid chromatography coupled with electrospray ionization tandem mass spectrometry.
PubMed:Modulatory effect of celastrol on Th1/Th2 cytokines profile, TLR2 and CD3+ T-lymphocyte expression in a relapsing-remitting model of multiple sclerosis in rats.
PubMed:Release of Ca2+ from the endoplasmic reticulum and its subsequent influx into mitochondria trigger celastrol-induced paraptosis in cancer cells.
PubMed:Celastrol induces unfolded protein response-dependent cell death in head and neck cancer.
PubMed:miR-326-histone deacetylase-3 feedback loop regulates the invasion and tumorigenic and angiogenic response to anti-cancer drugs.
PubMed:Celastrol may have an anti-atherosclerosis effect in a rabbit experimental carotid atherosclerosis model.
PubMed:Celastrol inhibits lung infiltration in differential syndrome animal models by reducing TNF-α and ICAM-1 levels while preserving differentiation in ATRA-induced acute promyelocytic leukemia cells.
PubMed:Celastrol attenuates inflammatory and neuropathic pain mediated by cannabinoid receptor type 2.
PubMed:Stemness is Derived from Thyroid Cancer Cells.
PubMed:Celastrol ameliorates HIV-1 Tat-induced inflammatory responses via NF-kappaB and AP-1 inhibition and heme oxygenase-1 induction in astrocytes.
PubMed:Accumulation of heme oxygenase-1 (HSP32) in Xenopus laevis A6 kidney epithelial cells treated with sodium arsenite, cadmium chloride or proteasomal inhibitors.
PubMed:Celastrol ameliorates cytokine toxicity and pro-inflammatory immune responses by suppressing NF-κB activation in RINm5F beta cells.
PubMed:Novel celastrol derivatives inhibit the growth of hepatocellular carcinoma patient-derived xenografts.
PubMed:Celastrol protects ischaemic myocardium through a heat shock response with up-regulation of haeme oxygenase-1.
PubMed:Design, synthesis and biological evaluation of C6-modified celastrol derivatives as potential antitumor agents.
PubMed:[Protective effect of celastrol on allergic rhinitis in rats].
PubMed:Celastrol enhanced the anticancer effect of lapatinib in human hepatocellular carcinoma cells in vitro.
PubMed:The effect of celastrol, a triterpene with antitumorigenic activity, on conformational and functional aspects of the human 90kDa heat shock protein Hsp90α, a chaperone implicated in the stabilization of the tumor phenotype.
PubMed:Solid self-microemulsifying dispersible tablets of celastrol: formulation development, charaterization and bioavailability evaluation.
PubMed:Taxodione and arenarone inhibit farnesyl diphosphate synthase by binding to the isopentenyl diphosphate site.
PubMed:Therapeutic inducers of the HSP70/HSP110 protect mice against traumatic brain injury.
PubMed:Celastrol inhibits the HIF-1α pathway by inhibition of mTOR/p70S6K/eIF4E and ERK1/2 phosphorylation in human hepatoma cells.
PubMed:The systemic amyloid precursor transthyretin (TTR) behaves as a neuronal stress protein regulated by HSF1 in SH-SY5Y human neuroblastoma cells and APP23 Alzheimer's disease model mice.
PubMed:Lack of neuroprotective effect of celastrol under conditions of proteasome inhibition by lactacystin in in vitro and in vivo studies: implications for Parkinson's disease.
PubMed:Celastrol targets proteostasis and acts synergistically with a heat-shock protein 90 inhibitor to kill human glioblastoma cells.
PubMed:NF-kappa B modulation is involved in celastrol induced human multiple myeloma cell apoptosis.
PubMed:Inhibition of autophagy strengthens celastrol-induced apoptosis in human pancreatic cancer in vitro and in vivo models.
PubMed:Alteration of the proteostasis network of plant cells promotes the post-endoplasmic reticulum trafficking of recombinant mutant (L444P) human β-glucocerebrosidase.
PubMed:Localization of heat shock proteins in cerebral cortical cultures following induction by celastrol.
PubMed:Celastrol enhances cell viability and inhibits amyloid-β production induced by lipopolysaccharide in vitro.
PubMed:Celastrol inhibits gastric cancer growth by induction of apoptosis and autophagy.
PubMed:Celastrol blocks interleukin-6 gene expression via downregulation of NF-κB in prostate carcinoma cells.
PubMed:Celastrol induces apoptosis in gefitinib-resistant non-small cell lung cancer cells via caspases-dependent pathways and Hsp90 client protein degradation.
PubMed:Evaluation of anticancer activity of celastrol liposomes in prostate cancer cells.
PubMed:Simultaneous NF-κB inhibition and E-cadherin upregulation mediate mutually synergistic anticancer activity of celastrol and SAHA in vitro and in vivo.
PubMed:Peptide deformylase inhibitor actinonin reduces celastrol's HSP70 induction while synergizing proliferation inhibition in tumor cells.
PubMed:A new multicolor bioluminescence imaging platform to investigate NF-κB activity and apoptosis in human breast cancer cells.
PubMed:Pristimerin enhances recombinant adeno-associated virus vector-mediated transgene expression in human cell lines in vitro and murine hepatocytes in vivo.
PubMed:Celastrol induces apoptosis of gastric cancer cells by miR-21 inhibiting PI3K/Akt-NF-κB signaling pathway.
PubMed:Celastrol ameliorates murine colitis via modulating oxidative stress, inflammatory cytokines and intestinal homeostasis.
PubMed:Celastrol increases glucocerebrosidase activity in Gaucher disease by modulating molecular chaperones.
PubMed:Plants and phytochemicals for Huntington's disease.
PubMed:Cancerous inhibitor of PP2A is targeted by natural compound celastrol for degradation in non-small-cell lung cancer.
PubMed:IP-FCM platform detects the existence and regulator-caused dissociation of components in naturally assembled HSP90 complex.
PubMed:Celastrol from 'Thunder God Vine' protects SH-SY5Y cells through the preservation of mitochondrial function and inhibition of p38 MAPK in a rotenone model of Parkinson's disease.
PubMed:Celastrol inhibits lipopolysaccharide-induced angiogenesis by suppressing TLR4-triggered nuclear factor-kappa B activation.
PubMed:Anti-invasive effects of celastrol in hypoxia-induced fibroblast-like synoviocyte through suppressing of HIF-1α/CXCR4 signaling pathway.
PubMed:Inhibitory effects of celastrol on rat liver cytochrome P450 1A2, 2C11, 2D6, 2E1 and 3A2 activity.
PubMed:[Chemical constituents of roots of Celastrus orbiculatus].
PubMed:Celastrol prevents cadmium-induced neuronal cell death via targeting JNK and PTEN-Akt/mTOR network.
PubMed:Association of heat-shock proteins in various neurodegenerative disorders: is it a master key to open the therapeutic door?
PubMed:Expression and purification of recombinant NRL-Hsp90α and Cdc37-CRL proteins for in vitro Hsp90/Cdc37 inhibitors screening.
PubMed:Testing agents for prevention or reversal of type 1 diabetes in rodents.
PubMed:miR-224 is critical for celastrol-induced inhibition of migration and invasion of hepatocellular carcinoma cells.
PubMed:Celastrol protects kidney against ischemia-reperfusion-induced injury in rats.
PubMed:Natural friedelanes.
PubMed:Chinese herbal medicine-derived compounds for cancer therapy: a focus on hepatocellular carcinoma.
PubMed:Celastrol inhibits lipopolysaccharide-stimulated rheumatoid fibroblast-like synoviocyte invasion through suppression of TLR4/NF-κB-mediated matrix metalloproteinase-9 expression.
PubMed:Celastrol inhibits TGF-β1-induced epithelial-mesenchymal transition by inhibiting Snail and regulating E-cadherin expression.
PubMed:ER stress-mediated apoptosis induced by celastrol in cancer cells and important role of glycogen synthase kinase-3β in the signal network.
PubMed:Prevention and Treatment of Colorectal Cancer by Natural Agents From Mother Nature.
PubMed:Inhibition of C2C12 myotube atrophy by a novel HSP70 inducer, celastrol, via activation of Akt1 and ERK1/2 pathways.
PubMed:Celastrol prevents atherosclerosis via inhibiting LOX-1 and oxidative stress.
PubMed:Celastrol and attenuation of tumor growth in systemic malignancies: a clinical perspective.
PubMed:Role of the eIF4E binding protein 4E-BP1 in regulation of the sensitivity of human pancreatic cancer cells to TRAIL and celastrol-induced apoptosis.
PubMed:Regiochemistry discoveries in the use of isoxazole as a handle for the rapid construction of an all-carbon macrocyclic precursor in the synthetic studies of celastrol.
PubMed:Celastrol induced DNA damage, cell cycle arrest, and apoptosis in human rheumatoid fibroblast-like synovial cells.
PubMed:Celastrol induces apoptosis of gastric cancer cells by miR-146a inhibition of NF-κB activity.
PubMed:Celastrol exerts synergistic effects with PHA-665752 and inhibits tumor growth of c-Met-deficient hepatocellular carcinoma in vivo.
PubMed:Celastrol, an NF-κB inhibitor, improves insulin resistance and attenuates renal injury in db/db mice.
PubMed:Celastrol protects human neuroblastoma SH-SY5Y cells from rotenone-induced injury through induction of autophagy.
PubMed:Heterogeneity in the properties of NEFL mutants causing Charcot-Marie-Tooth disease results in differential effects on neurofilament assembly and susceptibility to intervention by the chaperone-inducer, celastrol.
PubMed:Hsp70 silencing with siRNA in nanocarriers enhances cancer cell death induced by the inhibitor of Hsp90.
PubMed:Celastrol suppresses tumor cell growth through targeting an AR-ERG-NF-κB pathway in TMPRSS2/ERG fusion gene expressing prostate cancer.
PubMed:Identification of novel dietary phytochemicals inhibiting the efflux transporter breast cancer resistance protein (BCRP/ABCG2).
PubMed:Proteasome inhibition protects human peripheral blood mononuclear cells from radiation-induced oxidative stress.
PubMed:Phenotypic identification of the redox dye methylene blue as an antagonist of heat shock response gene expression in metastatic melanoma cells.
PubMed:Celastrol, an inhibitor of heat shock protein 90β potently suppresses the expression of matrix metalloproteinases, inducible nitric oxide synthase and cyclooxygenase-2 in primary human osteoarthritic chondrocytes.
PubMed:The extent of neurodegeneration and neuroprotection in two chemical in vitro models related to Parkinson's disease is critically dependent on cell culture conditions.
PubMed:Upregulating Noxa by ER stress, celastrol exerts synergistic anti-cancer activity in combination with ABT-737 in human hepatocellular carcinoma cells.
PubMed:Celastrol suppresses breast cancer MCF-7 cell viability via the AMP-activated protein kinase (AMPK)-induced p53-polo like kinase 2 (PLK-2) pathway.
PubMed:AFM studied the effect of celastrol on β1 integrin-mediated HUVEC adhesion and migration.
PubMed:Effects of celastrol on human cervical cancer cells as revealed by ion-trap gas chromatography-mass spectrometry based metabolic profiling.
PubMed:Lipophilic stinging nettle extracts possess potent anti-inflammatory activity, are not cytotoxic and may be superior to traditional tinctures for treating inflammatory disorders.
PubMed:Celastrol inhibits growth and induces apoptotic cell death in melanoma cells via the activation ROS-dependent mitochondrial pathway and the suppression of PI3K/AKT signaling.
PubMed:Oral bioavailability and gender-related pharmacokinetics of celastrol following administration of pure celastrol and its related tablets in rats.
PubMed:Celastrol inhibits interleukin-17A-stimulated rheumatoid fibroblast-like synoviocyte migration and invasion through suppression of NF-κB-mediated matrix metalloproteinase-9 expression.
PubMed:Celastrol attenuates adipokine resistin-associated matrix interaction and migration of vascular smooth muscle cells.
PubMed:The therapeutic potential of pharmacological chaperones and proteosomal inhibitors, Celastrol and MG132 in the treatment of sialidosis.
PubMed:Beta-catenin mediates the apoptosis induction effect of celastrol in HT29 cells.
PubMed:Induction of heat shock proteins in cerebral cortical cultures by celastrol.
PubMed:Suppression of autoimmune arthritis by Celastrus-derived Celastrol through modulation of pro-inflammatory chemokines.
PubMed:Optimized preparation of celastrol-loaded polymeric nanomicelles using rotatable central composite design and response surface methodology.
PubMed:Celastrol inhibits vasculogenesis by suppressing the VEGF-induced functional activity of bone marrow-derived endothelial progenitor cells.
PubMed:Strong inhibition of celastrol towards UDP-glucuronosyl transferase (UGT) 1A6 and 2B7 indicating potential risk of UGT-based herb-drug interaction.
PubMed:[Expression, purification of proteasome subunit PSMB1 and application in screening of possible proteasome inhibitors].
PubMed:Triptolide inhibits the proliferation of prostate cancer cells and down-regulates SUMO-specific protease 1 expression.
PubMed:Microarray-based gene expression profiling reveals the mediators and pathways involved in the anti-arthritic activity of Celastrus-derived Celastrol.
PubMed:Antitumor activity of celastrol nanoparticles in a xenograft retinoblastoma tumor model.
PubMed:TGF-β and NF-κB signal pathway cross-talk is mediated through TAK1 and SMAD7 in a subset of head and neck cancers.
PubMed:Unifying mechanisms of action of the anticancer activities of triterpenoids and synthetic analogs.
PubMed:Protective effect of celastrol in rat cerebral ischemia model: down-regulating p-JNK, p-c-Jun and NF-κB.
PubMed:Myogenesis in dysferlin-deficient myoblasts is inhibited by an intrinsic inflammatory response.
PubMed:Celastrus and its bioactive celastrol protect against bone damage in autoimmune arthritis by modulating osteoimmune cross-talk.
PubMed:Development of B cells and erythrocytes is specifically impaired by the drug celastrol in mice.
PubMed:Modulation of inflammatory signaling and cytokine release from microglia by celastrol incorporated into dendrimer nanocarriers.
PubMed:Celastrol nanoparticles inhibit corneal neovascularization induced by suturing in rats.
PubMed:Effective treatment of rat adjuvant-induced arthritis by celastrol.
PubMed:Celastrol analogues as inducers of the heat shock response. Design and synthesis of affinity probes for the identification of protein targets.
PubMed:Celastrol suppresses growth and induces apoptosis of human hepatocellular carcinoma through the modulation of STAT3/JAK2 signaling cascade in vitro and in vivo.
PubMed:Preparation, characterization, and assessment of the antiglioma effects of liposomal celastrol.
PubMed:Celastrol decreases specificity proteins (Sp) and fibroblast growth factor receptor-3 (FGFR3) in bladder cancer cells.
PubMed:Terpenoids from root bark of Celastrus orbiculatus.
PubMed:Formulation and evaluation of celastrol-loaded liposomes.
PubMed:Remarkable stereospecific conjugate additions to the Hsp90 inhibitor celastrol.
PubMed:Targeting inflammatory pathways by triterpenoids for prevention and treatment of cancer.
PubMed:Quantitative proteomics reveals cellular targets of celastrol.
PubMed:Sodium arsenite and cadmium chloride induction of proteasomal inhibition and HSP accumulation in Xenopus laevis A6 kidney epithelial cells.
PubMed:Ultrasound-assisted ionic liquid dispersive liquid-liquid microextraction coupled with high performance liquid chromatography for sensitive determination of trace celastrol in urine.
PubMed:Celastrol-induced apoptosis in human HaCaT keratinocytes involves the inhibition of NF-κB activity.
PubMed:Diarylheptanoids from the seeds of Alpinia katsumadai as heat shock factor 1 inducers.
PubMed:Paraptosis accompanied by autophagy and apoptosis was induced by celastrol, a natural compound with influence on proteasome, ER stress and Hsp90.
PubMed:Celastrol inhibits aminoglycoside-induced ototoxicity via heat shock protein 32.
PubMed:Celastrol inhibits breast cancer cell invasion via suppression of NF-ĸB-mediated matrix metalloproteinase-9 expression.
PubMed:Quinone methide tripterine, celastrol, induces apoptosis in human myeloma cells via NF-κB pathway.
PubMed:Tripterygium wilfordii bioactive compounds as anticancer and anti-inflammatory agents.
PubMed:Celastrol inhibits tumor cell proliferation and promotes apoptosis through the activation of c-Jun N-terminal kinase and suppression of PI3 K/Akt signaling pathways.
PubMed:Celastrol inhibits Tat-mediated human immunodeficiency virus (HIV) transcription and replication.
PubMed:The main anticancer bullets of the Chinese medicinal herb, thunder god vine.
PubMed:Celastrol regulates innate immunity response via NF-κB and Hsp70 in human retinal pigment epithelial cells.
PubMed:New strategy of photodynamic treatment of TiO2 nanofibers combined with celastrol for HepG2 proliferation in vitro.
PubMed:Radiosensitization by celastrol is mediated by modification of antioxidant thiol molecules.
PubMed:Celastrol targets mitochondrial respiratory chain complex I to induce reactive oxygen species-dependent cytotoxicity in tumor cells.
PubMed:Celastrol inhibits proliferation and induces chemosensitization through down-regulation of NF-κB and STAT3 regulated gene products in multiple myeloma cells.
PubMed:NADPH oxidase (NOX) isoforms are inhibited by celastrol with a dual mode of action.
PubMed:Gambogic acid, a natural product inhibitor of Hsp90.
PubMed:Celastrol induces apoptosis in non-small-cell lung cancer A549 cells through activation of mitochondria- and Fas/FasL-mediated pathways.
PubMed:[Effect of celastrol on Akt signaling pathway and apoptosis of leukemic K562 cell line].
PubMed:Celastrol induces expression of heme oxygenase-1 through ROS/Nrf2/ARE signaling in the HaCaT cells.
PubMed:Celastrus-derived celastrol suppresses autoimmune arthritis by modulating antigen-induced cellular and humoral effector responses.
PubMed:Tunable physiologic interactions of adhesion molecules for inflamed cell-selective drug delivery.
PubMed:Enhancement of radiation sensitivity in lung cancer cells by celastrol is mediated by inhibition of Hsp90.
PubMed:Inhibitory action of Celastrol on hypoxia-mediated angiogenesis and metastasis via the HIF-1α pathway.
PubMed:Shp2 protein tyrosine phosphatase inhibitor activity of estramustine phosphate and its triterpenoid analogs.
PubMed:Natural proteasome inhibitor celastrol suppresses androgen-independent prostate cancer progression by modulating apoptotic proteins and NF-kappaB.
PubMed:Molecular targets of celastrol derived from Thunder of God Vine: potential role in the treatment of inflammatory disorders and cancer.
PubMed:Phosphorylation and polyubiquitination of transforming growth factor beta-activated kinase 1 are necessary for activation of NF-kappaB by the Kaposi's sarcoma-associated herpesvirus G protein-coupled receptor.
PubMed:Celastrol isolated from Tripterygium regelii induces apoptosis through both caspase-dependent and -independent pathways in human breast cancer cells.
PubMed:A systematic protocol for the characterization of Hsp90 modulators.
PubMed:Anticancer activity of Celastrol in combination with ErbB2-targeted therapeutics for treatment of ErbB2-overexpressing breast cancers.
PubMed:PP2A mediated AMPK inhibition promotes HSP70 expression in heat shock response.
PubMed:Toxic effects of celastrol on embryonic development of zebrafish (Danio rerio).
PubMed:Celastrol inhibits the growth of estrogen positive human breast cancer cells through modulation of estrogen receptor α.
PubMed:Celastrol enhances AAV1-mediated gene expression in mice adipose tissues.
PubMed:Celastrol suppresses invasion of colon and pancreatic cancer cells through the downregulation of expression of CXCR4 chemokine receptor.
PubMed:Regulation of survival, proliferation, invasion, angiogenesis, and metastasis of tumor cells through modulation of inflammatory pathways by nutraceuticals.
PubMed:[Celastrol down-regulates expression of P-Akt and cyclin D1 in HL-60 cells and induces apoptosis].
PubMed:Cognitive decline following major surgery is associated with gliosis, β-amyloid accumulation, and τ phosphorylation in old mice.
PubMed:A cellular viability assay to monitor drug toxicity.
PubMed:Targeting apoptosis pathways in cancer by Chinese medicine.
PubMed:Small molecule inhibitors of IkappaB kinase signaling inhibit osteoclast formation in vitro and prevent ovariectomy-induced bone loss in vivo.
PubMed:Celastrol: a new therapeutic potential of traditional Chinese medicine.
PubMed:Synthesis and preliminary evaluation of neuroprotection of celastrol analogues in PC12 cells.
PubMed:Up-regulation of death receptor 4 and 5 by celastrol enhances the anti-cancer activity of TRAIL/Apo-2L.
PubMed:Celastrol suppresses IFN-gamma-induced ICAM-1 expression and subsequent monocyte adhesiveness via the induction of heme oxygenase-1 in the HaCaT cells.
PubMed:Celastrol regulates multiple nuclear transcription factors belonging to HSP90's clients in a dose- and cell type-dependent way.
PubMed:Celastrol acts as a potent antimetastatic agent targeting beta1 integrin and inhibiting cell-extracellular matrix adhesion, in part via the p38 mitogen-activated protein kinase pathway.
PubMed:Natural product Celastrol destabilizes tubulin heterodimer and facilitates mitotic cell death triggered by microtubule-targeting anti-cancer drugs.
PubMed:Celastrol attenuates hypertension-induced inflammation and oxidative stress in vascular smooth muscle cells via induction of heme oxygenase-1.
PubMed:HSP90 inhibitor, celastrol, arrests human monocytic leukemia cell U937 at G0/G1 in thiol-containing agents reversible way.
PubMed:Celastrol suppresses morphological and transcriptional responses in microglial cells upon stimulation with double-stranded RNA.
PubMed:Effects of Celastrol on growth inhibition of U937 leukemia cells through the regulation of the Notch1/NF-kappaB signaling pathway in vitro.
PubMed:Celastrol: Molecular targets of Thunder God Vine.
PubMed:Reduction of beta-amyloid pathology by celastrol in a transgenic mouse model of Alzheimer's disease.
PubMed:Celastrol can inhibit proteasome activity and upregulate the expression of heat shock protein genes, hsp30 and hsp70, in Xenopus laevis A6 cells.
PubMed:SARS-CoV 3CLpro inhibitory effects of quinone-methide triterpenes from Tripterygium regelii.
PubMed:Celastrol suppresses angiogenesis-mediated tumor growth through inhibition of AKT/mammalian target of rapamycin pathway.
PubMed:Celastrol, a triterpene, enhances TRAIL-induced apoptosis through the down-regulation of cell survival proteins and up-regulation of death receptors.
PubMed:Celastrol and an EGCG pro-drug exhibit potent chemosensitizing activity in human leukemia cells.
PubMed:Pharmacogenomic approach reveals a role for the x(c)- cystine/glutamate antiporter in growth and celastrol resistance of glioma cell lines.
PubMed:Celastrol inhibits Hsp90 chaperoning of steroid receptors by inducing fibrillization of the Co-chaperone p23.
PubMed:Celastrol synergistically enhances temozolomide cytotoxicity in melanoma cells.
PubMed:Synergistic anti-cancer activity by the combination of TRAIL/APO-2L and celastrol.
PubMed:Celastrol causes apoptosis and cell cycle arrest in rat glioma cells.
PubMed:Characterization of celastrol to inhibit hsp90 and cdc37 interaction.
PubMed:Celastrol, a novel HSP90 inhibitor, depletes Bcr-Abl and induces apoptosis in imatinib-resistant chronic myelogenous leukemia cells harboring T315I mutation.
PubMed:The NF-kappa B inhibitor, celastrol, could enhance the anti-cancer effect of gambogic acid on oral squamous cell carcinoma.
PubMed:Triterpenoids as new promising anticancer drugs.
PubMed:Neuroprotective effects of compounds with antioxidant and anti-inflammatory properties in a Drosophila model of Parkinson's disease.
PubMed:Antiangiogenic effect of celastrol on the growth of human glioma: an in vitro and in vivo study.
PubMed:MT7, a novel compound from a combinatorial library, arrests mitosis via inhibiting the polymerization of microtubules.
PubMed:Pharmacologic inhibitors of IkappaB kinase suppress growth and migration of mammary carcinosarcoma cells in vitro and prevent osteolytic bone metastasis in vivo.
PubMed:Celastrol, a triterpene extracted from Tripterygium wilfordii Hook F, inhibits platelet activation.
PubMed:Molecular mechanism of inhibition of the human protein complex Hsp90-Cdc37, a kinome chaperone-cochaperone, by triterpene celastrol.
PubMed:Suppression of inflammatory responses by celastrol, a quinone methide triterpenoid isolated from Celastrus regelii.
PubMed:Celastrol potentiates radiotherapy by impairment of DNA damage processing in human prostate cancer.
PubMed:Celastrol suppresses allergen-induced airway inflammation in a mouse allergic asthma model.
PubMed:Celastrol binds to ERK and inhibits FcepsilonRI signaling to exert an anti-allergic effect.
PubMed:CAGE, a cancer/testis antigen, induces c-FLIP(L) and Snail to enhance cell motility and increase resistance to an anti-cancer drug.
PubMed:Activation of the heat shock response in a primary cellular model of motoneuron neurodegeneration-evidence for neuroprotective and neurotoxic effects.
PubMed:Heat shock protein 90 inhibitors suppress aryl hydrocarbon receptor-mediated activation of CYP1A1 and CYP1B1 transcription and DNA adduct formation.
PubMed:Antiangiogenic activity of Tripterygium wilfordii and its terpenoids.
PubMed:Calpain-mediated androgen receptor breakdown in apoptotic prostate cancer cells.
PubMed:Celastrol inhibits the growth of human glioma xenografts in nude mice through suppressing VEGFR expression.
PubMed:Discovery of agents that eradicate leukemia stem cells using an in silico screen of public gene expression data.
PubMed:High-performance liquid chromatography spectrometric analysis of tripterin in rat plasma.
PubMed:A novel Hsp90 inhibitor to disrupt Hsp90/Cdc37 complex against pancreatic cancer cells.
PubMed:Activation of heat shock and antioxidant responses by the natural product celastrol: transcriptional signatures of a thiol-targeted molecule.
PubMed:Inhibition of anthrax lethal toxin-induced cytolysis of RAW264.7 cells by celastrol.
PubMed:Antimitotic quinoid triterpenes from Maytenus chuchuhuasca.
PubMed:Celastrol inhibits production of nitric oxide and proinflammatory cytokines through MAPK signal transduction and NF-kappaB in LPS-stimulated BV-2 microglial cells.
PubMed:Preclinical studies of celastrol and acetyl isogambogic acid in melanoma.
PubMed:Celastrol inhibits polyglutamine aggregation and toxicity though induction of the heat shock response.
PubMed:Induction of heat shock proteins in differentiated human and rodent neurons by celastrol.
PubMed:Molecular understanding and modern application of traditional medicines: triumphs and trials.
PubMed:Heat shock proteins and protection of the nervous system.
PubMed:Celastrol, a novel triterpene, potentiates TNF-induced apoptosis and suppresses invasion of tumor cells by inhibiting NF-kappaB-regulated gene products and TAK1-mediated NF-kappaB activation.
PubMed:The tumor proteasome is a primary target for the natural anticancer compound Withaferin A isolated from "Indian winter cherry".
PubMed:Gene expression signature-based chemical genomic prediction identifies a novel class of HSP90 pathway modulators.
PubMed:Inhibition of NF-kappa B activation through targeting I kappa B kinase by celastrol, a quinone methide triterpenoid.
PubMed:Naturally occurring NF-kappaB inhibitors.
PubMed:Celastrol blocks neuronal cell death and extends life in transgenic mouse model of amyotrophic lateral sclerosis.
PubMed:Neuroprotective agents for clinical trials in ALS: a systematic assessment.
PubMed:Celastrol, a triterpene extracted from the Chinese "Thunder of God Vine," is a potent proteasome inhibitor and suppresses human prostate cancer growth in nude mice.
PubMed:Chronic inhibition of cardiac Kir2.1 and HERG potassium channels by celastrol with dual effects on both ion conductivity and protein trafficking.
PubMed:Celastrol protects against MPTP- and 3-nitropropionic acid-induced neurotoxicity.
PubMed:Reversal of a full-length mutant huntingtin neuronal cell phenotype by chemical inhibitors of polyglutamine-mediated aggregation.
PubMed:Antifungal properties of pristimerin and celastrol isolated from Celastrus hypoleucus.
PubMed:Celastrols as inducers of the heat shock response and cytoprotection.
PubMed:Celastrol inhibits pro-inflammatory cytokine secretion in Crohn's disease biopsies.
PubMed:Preparative isolation and purification of celastrol from Celastrus orbiculatus Thunb. by a new counter-current chromatography method with an upright coil planet centrifuge.
PubMed:Antitumor agents. 228. five new agarofurans, Reissantins A-E, and cytotoxic principles from Reissantia buchananii.
PubMed:[Celastrol in the inhibition of neovascularization].
PubMed:Apoptosis induction in HL-60 cells and inhibition of topoisomerase II by triterpene celastrol.
PubMed:Effects of demethylzeylasteral and celastrol on spermatogenic cell Ca2+ channels and progesterone-induced sperm acrosome reaction.
PubMed:[Several monomes from Tripterygium wilfordii inhibit proliferation of glioma cells in vitro].
PubMed:Quantitative determination for cytotoxic Friedo-nor-oleanane derivatives from five morphological types of Maytenus ilicifolia (Celastraceae) by reverse-phase high-performance liquid chromatography.
PubMed:Antiinflammatory constituents of Celastrus orbiculatus inhibit the NF-kappaB activation and NO production.
PubMed:Celastrol, a potent antioxidant and anti-inflammatory drug, as a possible treatment for Alzheimer's disease.
PubMed:Immunomodulating components from chinese medicines.
PubMed:Novel quinone methides from Salacia kraussii with in vitro antimalarial activity.
PubMed:[In vitro inhibition of celastrol on spermatozoa fertilization ability of guinea pig].
PubMed:Structural basis of potent antiperoxidation activity of the triterpene celastrol in mitochondria: effect of negative membrane surface charge on lipid peroxidation.
PubMed:Quinone-methide triterpenes and salaspermic acid from Kokoona ochracea.
PubMed:Some progress on the chemistry of natural bioactive terpenoids from Chinese medicinal plants.
PubMed:The triterpene celastrol as a very potent inhibitor of lipid peroxidation in mitochondria.
PubMed:The cathedulin alkaloids.
 
Notes:
isolated from tripterygium wilfordii; potent inhibitory activity on both kir2.1 and erg1 potassium channels, leading to long qt syndrome. Celastrol, a plant-derived triterpene, has antioxidant and anti-inflammatory activity that may prevent neuronal degeneration in Alzheimer's disease (AD). In the brains of patients with AD signs of neuronal degeneration are accompanied by markers of microglial activation, inflammation, and oxidant damage. The presence of nitrotyrosine in the cell bodies of neurons in AD suggests that peroxynitrite contributes to the pathogenesis of the disease. In low nanomolar concentrations celastrol was found to suppress the production by human monocytes and macrophages of the pro-inflammatory cytokines TNF-alpha and IL-1beta. Celastrol also decreased the induced expression of class II MHC molecules by microglia. In macrophage lineage cells and endothelial cells celastrol decreased induced but not constitutive NO production. Celastrol suppresses adjuvant arthritis in the rat, demonstrating in vivo anti-inflammatory activity. Low doses of celastrol administered to rats significantly improved their performance in memory, learning and psychomotor activity tests. The potent antioxidant and anti-inflammatory activities of celastrol, and its effects on cognitive functions, suggest that the drug may be useful to treat neurodegenerative diseases accompanied by inflammation, such as AD. (PMID: 11513350) [HMDB]
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