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Celastrol Proteasome inhibiteur

Name: Celastrol
Brand: Selleck Chemicals
SKU: S1290
Rating: 5 (26 reviews)

N° Cat.S1290

Celastrol est un puissant inhibiteur de proteasome pour l'activité chymotrypsine-like d'un protéasome 20S purifié avec une IC50 de 2,5 μM. Ce composé induit l'apoptosis et l'autophagy via la voie de signalisation ROS/JNK. Il inhibe la mort neuronale dopaminergique de la maladie de Parkinson en activant la mitophagy.

Celastrol Proteasome inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 450.61

Aller à

Contrôle qualité

Lot : Pureté : 99.64%

99.64

Cibles apparentées	HDAC Caspase Secretase MMP HCV Protease Cysteine Protease DPP Tyrosinase HIV Protease Serine Protease
Autre Proteasome Inhibiteurs	MG132 Epoxomicin (BU-4061T) ONX-0914 (PR-957) Oprozomib Delanzomib VR23 Marizomib (Salinosporamide A) PI-1840 KSQ-4279 (USP1-IN-1) Isoginkgetin

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Concentration	Temps dincubation	Description de lactivité	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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Informations chimiques, stockage et stabilité

Poids moléculaire	450.61	Formule	C₂₉H₃₈O₄	Stockage (À partir de la date de réception)	3 ans-20°Cpoudre
N° CAS	34157-83-0	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	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

Solubilité

In vitro
Lot:

DMSO : 90 mg/mL (199.72 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

Ethanol : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	4.500mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 90 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	1.100mg/ml (2.44mM)	Taking the 1 mL working solution as an example, add 50 μL of 22 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Entrez les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre danimaux :

Étape 2 : Entrez la formulation in vivo (Ceci nest que le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuiteμL PEG300, mélanger et clarifier, ajouter ensuiteμL Tween 80, mélanger et clarifier, ajouter ensuite μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuite μL Huile de maïs, mélanger et clarifier.

Remarque : 1. Assurez-vous que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue lors de lajout précédent est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

Fonctionnalités	A potent antioxidant and anti-inflammatory drug.
Targets/IC₅₀/Ki	20S proteasome (Cell-free assay) 2.5 μM
In vitro	Celastrol à 5 μM inhibe les activités chymotrypsine-like, PGPH-like et trypsine-like du protéasome 20S purifié de 80%, 5% et <1% respectivement, tandis qu'à 10 μM, il inhibe ces trois activités protéasomales d'environ 90%, 15% et <1% respectivement. Ce composé inhibe significativement l'activité chymotrypsine protéasomale dans les cellules PC-3 de manière concentration-dépendante. Il induit à 2,5 μM à 5 μM l'activité caspase-3 de 4,7 à 5,5 fois dans les cellules PC-3. Dans ces cellules traitées chimiquement (5 μM), les niveaux des protéines cibles du proteasome, IκB-α et Bax, augmentent après 1 heure et continuent d'augmenter pour atteindre leur pic pendant 4 à 12 heures. Ce composé (2,5 μM) induit une inhibition du proteasome de 40%, comme le montrent la diminution des niveaux d'activité chymotrypsine-like et l'accumulation accrue de protéines ubiquitylées dans les cellules LNCaP. Il (2,5 μM) induit l'apoptosis dans les cellules LNCaP traitées au Celastrol, comme le montrent l'augmentation des niveaux d'activité caspase-3 (jusqu'à 3,5 fois), le clivage de PARP et la morphologie apoptotique. Ce composé (300 nM) supprime la production de TNF-alpha et d'IL-1beta induite par le LPS par les monocytes et les macrophages humains. Il (100 nM) diminue également l'expression des molécules de CMH de classe II induite par le LPS par la microglie. Ce produit chimique inhibe fortement la production de NO induite par le LPS et l'IFN-γ avec une IC50 de 200 nM dans les cellules de lignée macrophagique. Il inhibe fortement la production de NO induite par le TNF-α et l'IFN-γ avec une IC50 de 200 nM dans les cellules endothéliales. Ce composé (2,5 μM) potentialise l'apoptosis induite par le TNF et les agents chimiothérapeutiques et inhibe l'invasion, toutes deux régulées par l'activation de NF-kappaB, dans les cellules KBM-5. Il (2,5 μM) supprime l'expression des produits géniques induits par le TNF et impliqués dans l'antiapoptosis (IAP1, IAP2, Bcl-2, Bcl-XL, c-FLIP et survivin), la prolifération (cycline D1 et COX-2), l'invasion (MMP-9) et l'angiogenèse (VEGF) dans les cellules KBM-5. Ce produit chimique (5 μM) inhibe l'activation de la kinase IkappaBalpha induite par le TNF, la phosphorylation de IkappaBalpha, la dégradation de IkappaBalpha, la translocation nucléaire et la phosphorylation de p65, et l'expression du gène rapporteur médiée par NF-kappaB. Il inhibe la prolifération des cellules RPMI 8226, KATOIII, UM-SCC1, U251MG et MDA-MB-231 avec une IC50 de 0,52 μM, 0,54 μM, 0,76 μM, 0,69 μM et 0,67 μM, respectivement. Ce composé (1 μM) inhibe la croissance des RPMI 8226 avec une diminution des niveaux de cycline D1 et de cycline E, mais une augmentation concomitante des niveaux de p21 et p27. Il induit l'apoptosis dans les cellules RPMI-8226, comme l'indique l'activation de la caspase-8, le clivage de bid, l'activation de la caspase-9, l'activation de la caspase-3, le clivage de PARP et la régulation négative des protéines anti-apoptotiques. Ce produit chimique (1 μM) supprime la voie Akt et active la kinase JNK dans les cellules RPMI-8226.
Kinase Assay	Inhibition de l'activité du protéasome 20S purifié
Kinase Assay	Un protéasome 20S de lapin purifié (0,1 μg) est incubé avec 40 μM de divers substrats peptidiques fluorogènes dans 100 μL de tampon d'essai (20 mM Tris-HCl (pH 7,5)), en présence de Celastrol à différentes concentrations ou dans le solvant DMSO pendant 2 heures à 37 ℃, suivi de la mesure de l'inhibition de chaque activité protéasomale.
In vivo	Le Celastrol (3 mg/kg) entraîne une inhibition significative (jusqu'à 70%) de la croissance tumorale chez des souris nues mâles porteuses de tumeurs PC-3, associée à une augmentation des niveaux de p27 et de Bax. Ce composé entraîne davantage de cellules tumorales apoptotiques avec l'apparition de divers fragments de clivage de PARP dans la tumeur de souris nues mâles porteuses de tumeurs PC-3. Il provoque 35% d'inhibition tumorale, associée à une diminution de l'activité du protéasome et à une diminution de l'expression de la protéine AR chez des souris nues porteuses de tumeurs C4-2B. Ce produit chimique supprime fortement l'œdème articulaire et d'autres manifestations de l'arthrite adjuvante chez les souris. Il (0,2 mg/kg) améliore significativement les performances aux tests de mémoire, d'apprentissage et d'activité psychomotrice chez les rats.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/16651429/ [2] https://pubmed.ncbi.nlm.nih.gov/11513350/ [3] https://pubmed.ncbi.nlm.nih.gov/17110449/ [4] https://pubmed.ncbi.nlm.nih.gov/21786165/

Applications

Méthodes	Biomarqueurs	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	25383959
Immunofluorescence	p21 / Nur77	28388439
Growth inhibition assay	Cell viability	29040966

Informations sur lessai clinique

(données de https://clinicaltrials.gov, mis à jour le 2024-05-22)

Numéro NCT	Recrutement	Conditions	Sponsor/Collaborateurs	Date de début	Phases
NCT05494112	Recruiting	Safety	Legend Labz Inc.	May 25 2022	Not Applicable
NCT05413226	Recruiting	Safety Issues	Legend Labz Inc.	September 28 2021	Not Applicable

Support technique

Instructions de manipulation

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