Home Proteases Proteasome Inhibitor Celastrol

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Celastrol Proteasome Inhibitor

Kat.-Nr.S1290

Celastrol ist ein potenter Proteasom-Inhibitor für die chymotrypsinähnliche Aktivität eines gereinigten 20S Proteasoms mit einer IC50 von 2,5 μM. Diese Verbindung induziert Apoptosis und Autophagy über den ROS/JNK-Signalweg. Sie hemmt den dopaminergen neuronalen Zelltod bei Parkinson durch Aktivierung von Mitophagy.
Celastrol Proteasome Inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 450.61

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Qualitätskontrolle

Charge: Reinheit: 99.64%
99.64

Zellkultur, Behandlung & Arbeitskonzentration

Zelllinien Assay-Typ Konzentration Inkubationszeit Formulierung Aktivitätsbeschreibung PMID
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production treated 3 hrs before LPS challenge assessed after 24 hrs by Griess reagent assay, IC50 = 0.23 μM. 11809076
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NF-kappaB activation treated 3 hrs before LPS challenge assessed after 24 hrs by SEAP reporter gene assay, IC50 = 0.27 μM. 11809076
RPMI8226 Growth inhibition assay Growth inhibition of human RPMI8226 cells, IC50 = 3 μM. 18164197
HeLa Function assay Inhibition of TNF-alpha-induced NF-kappaB activation in human HeLa cells by SEAP reporter gene assay, IC50 = 0.15 μM. 18841906
RAW264.7 Function assay Inhibition of LPS-induced NF-kappaB activation in mouse RAW264.7 cells by SEAP reporter gene assay, IC50 = 0.3 μM. 18841906
SH-SY5Y Function assay Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in human SH-SY5Y cells assessed as lactate dehydrogenase release, EC50 = 0.03764 μM. 19138859
HeLa Function assay 2 hrs Amplification of HSF1 transcriptional activity in human heat shock-induced HeLa cells assessed as granule formation treated 1 hr before heat shock challenge measured after 2 hrs without recovery time by immunocytochemical staining, EC50 = 1.1 μM. 19502057
SK-N-SH Cytotoxicity assay 72 hrs Cytotoxicity against human SK-N-SH cells after 72 hrs by MTS assay, CC50 = 1.6 μM. 19502057
HeLa Function assay 3 hrs Amplification of HSF1 transcriptional activity in human HeLa cells assessed as granule formation pretreated for 3 hrs by immunocytochemical staining, EC50 = 2.6 μM. 19502057
HeLa Cytotoxicity assay 72 hrs Cytotoxicity against human HeLa cells after 72 hrs by MTS assay, CC50 = 3 μM. 19502057
HeLa Function assay Inhibition of NF-kappaB activity in human HeLa cells by SEAP reporter assay, IC50 = 0.15 μM. 20469887
LNCAP Antitumor assay Antitumor activity against human LNCAP cells, IC50 = 2.5 μM. 20627556
PC12 Cytoprotective assay Cytoprotective activity against t-BPH-induced cell damage in rat PC12 cells assessed as cell viability, IC50 = 3.15 μM. 20627556
PC12 Cytoprotective assay 1.6 uM Cytoprotective activity against t-BPH-induced cell damage in rat PC12 cells assessed as cell viability at 1.6 uM 20627556
THP1 Apoptosis assay 24 hrs Induction of apoptosis in TRAIL-resistant human THP1 cells after 24 hrs by annexin-V staining, EC50 = 15 μM. 20864342
293T Function assay 30 mins Inhibition of LPS-induced NF-kappaB activation in human 293T cells incubated for 30 mins followed by treated with LPS for 6 hrs by dual-luciferase reporter assay, IC50 = 0.17 μM. 21393004
293T Cytotoxicity assay Cytotoxicity against human 293T cells assessed as cell viability by dual-luciferase reporter assay, IC50 = 0.67 μM. 21393004
RAW264 Function assay 24 hrs Inhibition of LPS-induced NO production in mouse RAW264 cells after 24 hrs 21393004
NCI-H460 Cytotoxicity assay Cytotoxicity against human NCI-H460 cells after overnight incubation by MTT assay, IC50 = 12.3 μM. 21942765
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess reagent method, IC50 = 1 μM. 21978676
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by griess assay, IC50 = 1 μM. 22024033
RAW264.7 Function assay 18 hrs Inhibition of LPS-stimulated NFkappaB activation transfected in mouse RAW264.7 cells after 18 hrs by luciferase reporter gene assay, IC50 = 0.2 μM. 22705020
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in CCR2 expression at 200 ug, ip starting from arthritis onset and continued uninterrupted until 22854193
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in GRO/KC production at 200 ug, ip starting from arthritis onset and continued uninterrupted unti 22854193
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in MCP1 production at 200 ug, ip starting from arthritis onset and continued uninterrupted until 22854193
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in RANTES production at 200 ug, ip starting from arthritis onset and continued uninterrupted unti 22854193
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in TNFalpha production at 200 ug, ip starting from arthritis onset and continued uninterrupted un 22854193
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in CCR3 expression at 200 ug, ip starting from arthritis onset and continued uninterrupted until 22854193
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in CCR6 expression at 200 ug, ip starting from arthritis onset and continued uninterrupted until 22854193
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in CXCR1 expression at 200 ug, ip starting from arthritis onset and continued uninterrupted until 22854193
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in CXCR2 expression at 200 ug, ip starting from arthritis onset and continued uninterrupted until 22854193
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in CXCR4 expression at 200 ug, ip starting from arthritis onset and continued uninterrupted until 22854193
spleen adherent cells Function assay 200 ug Increase in CCR1 expression in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation at 200 ug, ip starting from arthritis onset and continued uninterrupted until study end by qPCR relative baselin 22854193
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in IL-1beta production at 200 ug, ip starting from arthritis onset and continued uninterrupted un 22854193
spleen adherent cells Antiarthritic assay 200 ug Antiarthritic effect in Lewis rat adjuvant-induced arthritis model spleen adherent cells restimulated with sonicated Mtb post isolation assessed as reduction in CCR5 expression at 200 ug, ip starting from arthritis onset and continued uninterrupted until 22854193
spleen adherent cells Function assay 24 hrs Increase in CCR1 protein surface expression in sonicated Mtb-stimulated spleen adherent cells isolated from Lewis rat adjuvant-induced arthritis model pre-incubated with 0.1 to 0.3 uM compound before stimulation with sonicated Mtb for 24 hrs by flow cytom 22854193
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess method, IC50 = 1 μM. 23127886
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production incubated for 24 hrs by ELISA, IC50 = 0.8 μM. 23234407
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide generation incubated for 24 hrs, IC50 = 1 μM. 23234407
RAW264.7 Antiinflammatory assay Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production by Griess reaction based method, IC50 = 1 μM. 25637363
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay, IC50 = 0.153 μM. 25756299
MCF7 Function assay 24 hrs Inhibition of HSP90 in human MCF7 cells assessed as pAkt degradation at 5 times IC50 after 24 hrs by Western blot analysis 25756299
MCF7 Function assay 24 hrs Inhibition of HSP90 in human MCF7 cells assessed as Her2 degradation at 5 times IC50 after 24 hrs by Western blot analysis 25756299
MCF7 Function assay 24 hrs Inhibition of HSP90 in human MCF7 cells assessed as Cdk6 degradation at 5 times IC50 after 24 hrs by Western blot analysis 25756299
MCF7 Function assay 24 hrs Inhibition of HSP90 in human MCF7 cells assessed as Raf degradation at 5 times IC50 after 24 hrs by Western blot analysis 25756299
MCF7 Function assay 24 hrs Change in Cdc37 expression in human MCF7 cells at 5 times IC50 after 24 hrs by Western blot analysis 25756299
MCF7 Function assay 24 hrs Change in p23 expression in human MCF7 cells at 5 times IC50 after 24 hrs by Western blot analysis 25756299
MCF7 Function assay 24 hrs Inhibition of HSP90 in human MCF7 cells assessed as disruption of interaction with Cdc37 at 5 times IC50 after 24 hrs by co-immunoprecipitation assay 25756299
MCF7 Function assay 24 hrs Inhibition of HSP90 in human MCF7 cells assessed as disruption of interaction with p23 at 5 times IC50 after 24 hrs by co-immunoprecipitation assay 25756299
SGC7901 Anticancer assay 48 hrs Anticancer activity against human SGC7901 cells assessed as cell survival after 48 hrs by MTT assay, IC50 = 0.15 μM. 25812966
SMMC7721 Anticancer assay 48 hrs Anticancer activity against human SMMC7721 cells assessed as cell survival after 48 hrs by MTT assay, IC50 = 0.58 μM. 25812966
MGC803 Anticancer assay 48 hrs Anticancer activity against human MGC803 cells assessed as cell survival after 48 hrs by MTT assay, IC50 = 1.55 μM. 25812966
HepG2 Anticancer assay 48 hrs Anticancer activity against human HepG2 cells assessed as cell survival after 48 hrs by MTT assay, IC50 = 4.01 μM. 25812966
A549 Antiproliferative assay 48 hrs Antiproliferative activity against paclitaxel-resistant human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 2.01 μM. 27647369
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 2.02 μM. 27647369
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 2.13 μM. 27647369
PANC1 Antiproliferative assay 48 hrs Antiproliferative activity against human PANC1 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50 = 2.48 μM. 27647369
LNCAP Function assay 5 uM 24 hrs Antagonist activity at AR in human LNCAP cells assessed as suppression of DHT-induced receptor transcriptional activity at 5 uM after 24 hrs by dual luciferase reporter gene assay 27994731
A549 Growth inhibition assay 6 days Growth inhibition of human A549 cells measured every 2 hrs over 6 days by live cell imaging based method, IC50 = 0.69 μM. 28621943
HEK293 Function assay 10 uM 20 mins Inhibition of Galphao interaction with GFP-fused RGS17 (unknown origin) deltaN mutant expressed in HEK293 cells assessed as increase in RGS17 deltaN mutant localization at cytoplasm at 10 uM up to 20 mins by confocal microscopic analysis 28621943
HEK293 Function assay 100 uM 5 mins Inhibition of Galpha0 interaction with GFP-fused RGS17 (unknown origin) deltaN mutant expressed in HEK293 cells assessed as increase in RGS17 deltaN mutant localization at cytoplasm at 100 uM up to 5 mins by confocal microscopic analysis 28621943
HEK293 Function assay 10 uM 5 mins Inhibition of Galphao interaction with GFP-fused RGS17 (unknown origin) deltaN mutant expressed in HEK293 cells assessed as increase in RGS17 deltaN mutant localization at cytoplasm at 10 uM up to 5 mins by confocal microscopic analysis 28621943
MIAPaCa2 Antiproliferative assay 72 hrs Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by MTT assay, IC50 = 0.46 μM. 28688281
SKBR3 Antiproliferative assay 72 hrs Antiproliferative activity against human SKBR3 cells after 72 hrs by MTT assay, IC50 = 0.72 μM. 28688281
SKOV3 Antiproliferative assay 72 hrs Antiproliferative activity against human SKOV3 cells after 72 hrs by MTT assay, IC50 = 1.16 μM. 28688281
MDA-MB-231 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 1.32 μM. 28688281
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 1.56 μM. 28688281
BJ Cytotoxicity assay 72 hrs Cytotoxicity against human BJ cells assessed as reduction in cell viability after 72 hrs by MTT assay, IC50 = 2.74 μM. 28688281
NCI-H460 Function assay 1 uM 12 hrs Activation of HSF1 in human NCI-H460 cells assessed as upregulation of HSP25 protein levels at 1 uM after 12 hrs by Western blot analysis 28737916
NCI-H460 Function assay 1 uM 12 hrs Activation of HSF1 in human NCI-H460 cells assessed as upregulation of HSP70 protein levels at 1 uM after 12 hrs by Western blot analysis 28737916
NCI-H1299 Cytotoxicity assay Cytotoxicity in human NCI-H1299 cells assessed as reduction in cell viability, IC50 = 1 μM. 28754470
BCP-ALL Cytotoxicity assay Cytotoxicity in human BCP-ALL cells assessed as reduction in cell viability, IC50 = 1 μM. 28754470
T-ALL Cytotoxicity assay Cytotoxicity in human T-ALL cells assessed as reduction in cell viability, IC50 = 1 μM. 28754470
Daudi Cytotoxicity assay Cytotoxicity in human Daudi cells assessed as reduction in cell viability, IC50 = 1 μM. 28754470
HL60 Cytotoxicity assay Cytotoxicity in human HL60 cells assessed as reduction in cell viability, IC50 = 1 μM. 28754470
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
fibroblast cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
HCT116 Antiproliferative assay 48 hrs Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay, IC50 = 5.26 μM. 29486954
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50 = 6.17 μM. 29486954
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 6.59 μM. 29486954
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 6.84 μM. 29486954
HEK293 Cytotoxicity assay Cytotoxicity against HEK293 cells (CO-ADD:MA_007); CC50 by cell viability assay in DMEM (10% FBS) media using TC plates, by Resazurin F(560/590), CC50 = 0.837 μM. ChEMBL
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Chemische Informationen, Lagerung & Stabilität

Molekulargewicht 450.61 Formel

C29H38O4

 Lagerung (Ab dem Eingangsdatum)
CAS-Nr. 34157-83-0 SDF herunterladen Lagerung von Stammlösungen

Synonyme NSC 70931, Tripterine Smiles CC1=C(C(=O)C=C2C1=CC=C3C2(CCC4(C3(CCC5(C4CC(CC5)(C)C(=O)O)C)C)C)C)O

Löslichkeit

In vitro
Charge:

DMSO : 90 mg/mL (199.72 mM)
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Water : Insoluble

Ethanol : Insoluble

Molaritätsrechner

Masse Konzentration Volumen Molekulargewicht
Verdünnungsrechner Molekulargewichtsrechner

In vivo
Charge:

In-vivo-Formulierungsrechner (Klare Lösung)

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Wirkmechanismus

Merkmale
A potent antioxidant and anti-inflammatory drug.
Targets/IC50/Ki
20S proteasome
(Cell-free assay)
2.5 μM
In vitro
Celastrol hemmt bei einer Konzentration von 5 μM die Chymotrypsin-, PGPH- und Trypsin-ähnlichen Aktivitäten des gereinigten 20S-Proteasoms um 80 %, 5 % bzw. <1 %, während es bei einer Konzentration von 10 μM diese drei Proteasomaktivitäten um ca. 90 %, 15 % bzw. <1 % hemmt. Es hemmt die proteasomale Chymotrypsinaktivität in PC-3-Zellen in konzentrationsabhängiger Weise signifikant. Bei 2,5 μM bis 5 μM induziert es die Caspase-3-Aktivität in PC-3-Zellen um das 4,7- bis 5,5-fache. In mit dieser Chemikalie (5 μM) behandelten Zellen sind die Konzentrationen der Proteasom-Zielproteine IκB-α und Bax nach 1 Stunde erhöht und steigen weiter an, bis sie nach 4 bis 12 Stunden ihren Höchstwert erreichen. Die Behandlung mit dieser Verbindung (2,5 μM) induziert eine Proteasom-Hemmung um 40 %, was sich in einer Abnahme der Chymotrypsin-ähnlichen Aktivität und einer erhöhten Akkumulation von ubiquitinierten Proteinen in LNCaP-Zellen zeigt. Es (2,5 μM) induziert Apoptose in den mit Celastrol behandelten LNCaP-Zellen, was sich in erhöhten Werten der Caspase-3-Aktivität (bis zum 3,5-Fachen), PARP-Spaltung und apoptotischer Morphologie zeigt. Es wurde festgestellt, dass diese Verbindung (300 nM) die LPS-induzierte Produktion von TNF-alpha und IL-1beta durch menschliche Monozyten und Makrophagen unterdrückt. Sie (100 nM) verringert auch die LPS-induzierte Expression von MHC-Molekülen der Klasse II durch Mikroglia. Diese Chemikalie hemmt stark die LPS- und IFN-y-induzierte NO-Produktion mit einer IC50 von 200 nM in Zellen der Makrophagenlinie. Sie hemmt stark die TNF-α- und IFN-γ-induzierte NO-Produktion mit einer IC50 von 200 nM in Endothelzellen.Diese Verbindung (2,5 μM) potenziert die durch TNF und Chemotherapeutika induzierte Apoptose und hemmt die Invasion, die beide durch die NF-κB-Aktivierung reguliert werden, in KBM-5-Zellen. Es (2,5 μM) unterdrückt die durch TNF induzierte Expression von Genprodukten, die an der Antiapoptose (IAP1, IAP2, Bcl-2, Bcl-XL, c-FLIP und Survivin), der Proliferation (Cyclin D1 und COX-2), der Invasion (MMP-9) und der Angiogenese (VEGF) in KBM-5-Zellen beteiligt sind. Es wurde festgestellt, dass diese Chemikalie (5 μM) die TNF-induzierte Aktivierung der IkappaBalpha-Kinase, die IkappaBalpha-Phosphorylierung, den IkappaBalpha-Abbau, die p65-Kern-Translokation und -Phosphorylierung sowie die NF-kappaB-vermittelte Reportergenexpression hemmt. Sie hemmt die Proliferation von RPMI 8226-, KATOIII-, UM-SCC1-, U251MG- und MDA-MB-231-Zellen mit einer IC50 von 0,52 μM, 0,54 μM, 0,76 μM, 0,69 μM bzw. 0,67 μM. Die Verbindung (1 μM) hemmt das Wachstum von RPMI 8226 mit einer Abnahme der Konzentrationen von Cyclin D1 und Cyclin E, aber einer gleichzeitigen Zunahme der Konzentrationen von p21 und p27. Es induziert Apoptose in RPMI-8226-Zellen, was durch die Aktivierung von Caspase-8, Bid-Spaltung, Caspase-9-Aktivierung, Caspase-3-Aktivierung, PARP-Spaltung und durch die Herunterregulierung von anti-apoptotischen Proteinen angezeigt wird. Die Substanz (1 μM) unterdrückt den Akt-Signalweg und aktiviert die JNK-Kinase in RPMI-8226-Zellen.
Kinase-Assay
Hemmung der Aktivität von gereinigtem 20S-Proteasom
Ein gereinigtes 20S-Proteasom aus Kaninchen (0,1 μg) wird mit 40 μM verschiedener fluorogener Peptidsubstrate in 100 μL Assay-Puffer (20 mM Tris-HCl (pH 7,5)) in Gegenwart von Celastrol in verschiedenen Konzentrationen oder im Lösungsmittel DMSO 2 Stunden lang bei 37 °C inkubiert, Anschließend wird die Hemmung der jeweiligen Proteasomaktivität gemessen.
In vivo
Celastrol (3 mg/kg) führt zu einer signifikanten Hemmung (bis zu 70 %) des Tumorwachstums bei männlichen Nacktmäusen mit PC-3-Tumoren, verbunden mit erhöhten p27- und Bax-Spiegeln. Es führt zu mehr apoptotischen Tumorzellen mit dem Auftreten verschiedener PARP-Spaltfragmente im Tumor von männlichen Nacktmäusen mit PC-3-Tumoren. Es bewirkt eine 35-prozentige Hemmung des Tumors, verbunden mit einer verminderten Proteasomaktivität und einer verminderten Expression des AR-Proteins in Nacktmäusen mit C4-2B-Tumoren.Es wurde festgestellt, dass diese Chemikalie Gelenkschwellungen und andere Manifestationen der Adjuvansarthritis bei Mäusen stark unterdrückt. Die Substanz (0,2 mg/kg) verbessert die Leistung in Gedächtnis-, Lern- und psychomotorischen Aktivitätstests bei Ratten signifikant.
Literatur
  • [4] https://pubmed.ncbi.nlm.nih.gov/21786165/

Anwendungen

Methoden Biomarker Bilder PMID
Western blot HIF-1α Akt / p-Akt / p-p70S6K PARP / p53 / p21 / cIAP1 / Bcl-xl / Bcl-2 IκBα / p-IKKα/β iNOS / COX-2 / Arg-1 Chk2 / p-Chk2 / Cyclin B1 / Cdc25c / p-Cdc25c
S1290-WB1
25383959
Immunofluorescence p21 / Nur77
S1290-IF1
28388439
Growth inhibition assay Cell viability
S1290-viability1
29040966

Klinische Studieninformationen

(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)

NCT-Nummer Rekrutierung Erkrankungen Sponsor/Kooperationspartner Startdatum Phasen
NCT05494112 Recruiting
Safety
Legend Labz Inc.
 May 25 2022 Not Applicable
NCT05413226 Recruiting
Safety Issues
Legend Labz Inc.
 September 28 2021 Not Applicable

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