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Celastrol (Tripterine) HSP90-middendomeinremmer

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

Cat.Nr.: S1290

Celastrol is een potente proteasome-remmer voor de chymotrypsine-achtige activiteit van een gezuiverd 20S proteasome met een IC50 van 2,5 μM. Celastrol induceert apoptosis en autophagy via de ROS/JNK-signaalroute. Celastrol remt de dopaminerge neuronale dood bij de ziekte van Parkinson door activering van mitophagy.

Celastrol (Tripterine) HSP Remmer Chemical Structure

Chemische structuur

Moleculair gewicht: 450.61

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.64%

99.64

Gerelateerde doelwitten	Akt Wnt/beta-catenin PKC ROCK Microtubule Associated Integrin Bcr-Abl Actin FAK Kinesin
Overige HSP Inhibitoren	Tanespimycin (17-AAG) Elesclomol (STA-4783) Luminespib (NVP-AUY922) Ganetespib (STA-9090) Alvespimycin (17-DMAG) Hydrochloride VER-155008 Onalespib (AT13387) BIIB021 Zelavespib (PU-H71) NVP-BEP800

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	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 informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Moleculair gewicht	450.61	Formule	C₂₉H₃₈O₄	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	34157-83-0	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	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

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 90 mg/mL (199.72 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	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.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

Kenmerken	A potent antioxidant and anti-inflammatory drug.
Targets/IC₅₀/Ki	20S proteasome (Cell-free assay) 2.5 μM
In vitro	Celastrol bij 5 μM remt de chymotrypsine-achtige, PGPH-achtige en trypsine-achtige activiteiten van het gezuiverde 20S proteasoom met respectievelijk 80%, 5% en <1%, terwijl bij 10 μM het deze drie proteasomale activiteiten remt met respectievelijk ~90%, 15% en <1%. Deze verbinding remt significant de proteasomale chymotrypsine-activiteit in PC-3-cellen op een concentratieafhankelijke manier. Het induceert bij 2,5 μM tot 5 μM de caspase-3-activiteit met 4,7-voudig tot 5,5-voudig in PC-3-cellen. In deze chemisch (5 μM) behandelde cellen stijgen de niveaus van de proteasome doelwitproteïnen, IκB-α en Bax, na 1 uur en stijgen verder tot hun piek gedurende 4 tot 12 uur. Deze verbinding (2,5 μM) behandeling induceert proteasome-remming met 40%, zoals aangetoond door de verlaagde niveaus van chymotrypsine-achtige activiteit en verhoogde accumulatie van ubiquitinated proteïnen in LNCaP-cellen. Het (2,5 μM) induceert apoptosis in de Celastrol-behandelde LNCaP-cellen, zoals aangetoond door verhoogde niveaus van caspase-3-activiteit (tot 3,5-voudig), PARP-splitsing en apoptotische morfologie. Van deze verbinding (300 nM) is gevonden dat het de LPS-geïnduceerde productie van TNF-alfa en IL-1beta door humane monocyten en macrofagen onderdrukt. Het (100 nM) vermindert ook de LPS-geïnduceerde expressie van klasse II MHC-moleculen door microglia. Deze chemische stof remt sterk de LPS- en IFN-y-geïnduceerde NO-productie met een IC50 van 200 nM in macrofaaglijncellen. Het remt sterk de TNF-α- en IFN-γ-geïnduceerde NO-productie met een IC50 van 200 nM in endotheelcellen. Deze verbinding (2,5 μM) versterkt de apoptosis geïnduceerd door TNF en chemotherapeutische middelen en remt invasie, beide gereguleerd door NF-kappaB-activering, in KBM-5-cellen. Het (2,5 μM) onderdrukt de expressie van TNF geïnduceerde expressie van genproducten betrokken bij antiapoptosis (IAP1, IAP2, Bcl-2, Bcl-XL, c-FLIP en survivin), proliferatie (cyclin D1 en COX-2), invasie (MMP-9) en angiogenese (VEGF) in KBM-5-cellen. Van deze chemische stof (5 μM) is gevonden dat het de TNF-geïnduceerde activering van IkappaBalpha kinase, IkappaBalpha fosforylering, IkappaBalpha afbraak, p65 nucleaire translocatie en fosforylering, en NF-kappaB-gemedieerde reportergenexpressie remt. Het remt de proliferatie van RPMI 8226, KATOIII, UM-SCC1, U251MG en MDA-MB-231-cellen met een IC50 van respectievelijk 0,52 μM, 0,54 μM, 0,76 μM, 0,69 μM en 0,67 μM. Deze verbinding (1 μM) remt de groei van RPMI 8226 met een afname van de niveaus van cyclin D1 en cyclin E, maar een gelijktijdige toename van de niveaus van p21 en p27. Het induceert apoptosis in RPMI-8226-cellen, aangegeven door de activering van caspase-8, bid-splitsing, caspase-9-activering, caspase-3-activering, PARP-splitsing en door de downregulatie van anti-apoptotische proteïnen. Deze chemische stof (1 μM) onderdrukt de Akt-route en activeert JNK-kinase in RPMI-8226-cellen.
Kinase Assay	Remming van gezuiverde 20S proteasome-activiteit
Kinase Assay	Een gezuiverd konijn 20S proteasome (0,1 μg) wordt geïncubeerd met 40 μM van verschillende fluorogene peptidesubstraten in 100 μL assaybuffer (20 mM Tris-HCl (pH 7.5)), in aanwezigheid van Celastrol in verschillende concentraties of in het oplosmiddel DMSO gedurende 2 uur bij 37 ℃, gevolgd door meting van de remming van elke proteasomale activiteit.
In vivo	Celastrol (3 mg/kg) resulteert in een significante remming (tot 70%) van tumorgroei bij mannelijke naakte muizen met PC-3-tumoren, geassocieerd met verhoogde p27-niveaus en Bax-niveaus. Deze verbinding resulteert in meer apoptotische tumorcellen met de verschijning van verschillende PARP-splitsingsfragmenten in tumoren van mannelijke naakte muizen met PC-3-tumoren. Het veroorzaakt 35% tumorremming, geassocieerd met verminderde proteasome-activiteit en verminderde expressie van AR-proteïne in naakte muizen met C4-2B-tumoren. Van deze chemische stof is gevonden dat het gewrichtszwelling en andere manifestaties van adjuvante artritis bij muizen sterk onderdrukt. Het (0,2 mg/kg) verbetert significant de prestaties in geheugen-, leer- en psychomotorische activiteitstests bij ratten.
Referenties	[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/

Toepassingen (Applications)

Methoden	Biomarkers	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

Informatie klinische proef (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
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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