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Celastrol Proteasome inhibidor

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

Cat. No.S1290

Celastrol es un potente inhibidor del proteasome para la actividad similar a la quimotripsina de un proteasome 20S purificado con una IC50 de 2,5 μM. Este compuesto induce apoptosis y autophagy a través de la vía de señalización ROS/JNK. Inhibe la muerte neuronal dopaminérgica de la enfermedad de Parkinson mediante la activación de la mitophagy.

Celastrol Proteasome inhibidor Chemical Structure

Estructura química

Peso molecular: 450.61

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Control de calidad

Lote: Pureza: 99.64%

99.64

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

Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Descripción de la actividad	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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Información química, almacenamiento y estabilidad

Peso molecular	450.61	Fórmula	C₂₉H₃₈O₄	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	34157-83-0	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	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

Solubilidad

In vitro
Lote:

DMSO : 90 mg/mL (199.72 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : Insoluble

Ethanol : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción

Características	A potent antioxidant and anti-inflammatory drug.
Targets/IC₅₀/Ki	20S proteasome (Cell-free assay) 2.5 μM
In vitro	Celastrol a 5 μM inhibe las actividades quimotripsina, PGPH y tripsina del proteasome 20S purificado en un 80 %, 5 % y <1 %, respectivamente, mientras que a 10 μM, inhibe estas tres actividades proteasomales en un ~90 %, 15 % y <1 %, respectivamente. Este compuesto inhibe significativamente la actividad quimotripsina proteasomal en células PC-3 de manera dependiente de la concentración. A 2,5 μM a 5 μM, induce la actividad de la caspasa-3 de 4,7 a 5,5 veces en células PC-3. En células tratadas con este químico (5 μM), los niveles de las proteínas diana del proteasome, IκB-α y Bax, aumentan después de 1 hora y se incrementan aún más hasta su pico durante 4 a 12 horas. Este compuesto (2,5 μM) induce una inhibición del proteasome del 40 %, como se muestra por la disminución de los niveles de actividad similar a la quimotripsina y el aumento de la acumulación de proteínas ubiquitinadas en células LNCaP. Induce (2,5 μM) apoptosis en las células LNCaP tratadas con Celastrol, como se muestra por el aumento de los niveles de actividad de la caspasa-3 (hasta 3,5 veces), el clivaje de PARP y la morfología apoptótica. Se ha descubierto que este compuesto (300 nM) suprime la producción de TNF-alfa e IL-1beta inducida por LPS por monocitos y macrófagos humanos. También (100 nM) disminuye la expresión de moléculas MHC de clase II inducida por LPS por la microglía. Este químico inhibe fuertemente la producción de NO inducida por LPS e IFN-γ con una IC50 de 200 nM en células de linaje de macrófagos. Inhibe fuertemente la producción de NO inducida por TNF-α e IFN-γ con una IC50 de 200 nM en células endoteliales. Este compuesto (2,5 μM) potencia la apoptosis inducida por TNF y agentes quimioterapéuticos e inhibe la invasión, ambas reguladas por la activación de NF-kappaB, en células KBM-5. Suprime (2,5 μM) la expresión de TNF inducida por la expresión de productos génicos involucrados en la antiapoptosis (IAP1, IAP2, Bcl-2, Bcl-XL, c-FLIP y survivina), la proliferación (ciclina D1 y COX-2), la invasión (MMP-9) y la angiogénesis (VEGF) en células KBM-5. Se ha descubierto que este químico (5 μM) inhibe la activación inducida por TNF de la IkappaBalpha quinasa, la fosforilación de IkappaBalpha, la degradación de IkappaBalpha, la translocación nuclear y la fosforilación de p65, y la expresión del gen reportero mediada por NF-kappaB. Inhibe la proliferación de células RPMI 8226, KATOIII, UM-SCC1, U251MG y MDA-MB-231 con una IC50 de 0,52 μM, 0,54 μM, 0,76 μM, 0,69 μM y 0,67 μM, respectivamente. Este compuesto (1 μM) inhibe el crecimiento de RPMI 8226 con una disminución en los niveles de ciclina D1 y ciclina E, pero un aumento concomitante en los niveles de p21 y p27. Induce apoptosis en células RPMI-8226, indicada por la activación de la caspasa-8, el clivaje de bid, la activación de la caspasa-9, la activación de la caspasa-3, el clivaje de PARP y la regulación a la baja de las proteínas antiapoptóticas. Este químico (1 μM) suprime la vía Akt y activa la quinasa JNK en células RPMI-8226.
Ensayo de quinasa	Inhibición de la actividad del proteasome 20S purificado
Ensayo de quinasa	Un proteasome 20S de conejo purificado (0,1 μg) se incuba con 40 μM de varios sustratos peptídicos fluorogénicos en 100 μL de tampón de ensayo (20 mM Tris-HCl (pH 7,5)), en presencia de Celastrol a diferentes concentraciones o en el disolvente DMSO durante 2 horas a 37 ℃, seguido de la medición de la inhibición de cada actividad proteasomal.
In vivo	Celastrol (3 mg/kg) produce una inhibición significativa (hasta un 70 %) del crecimiento tumoral en ratones nude machos con tumores PC-3, asociada con un aumento de los niveles de p27 y Bax. Este compuesto resulta en más células tumorales apoptóticas con la aparición de varios fragmentos de clivaje de PARP en tumores de ratones nude machos con tumores PC-3. Causa un 35 % de inhibición tumoral, asociada con una disminución de la actividad del proteasome y una disminución de la expresión de la proteína AR en ratones nude con tumores C4-2B. Se ha descubierto que este químico suprime fuertemente la hinchazón articular y otras manifestaciones de artritis adyuvante en ratones. A 0,2 mg/kg, mejora significativamente el rendimiento en pruebas de memoria, aprendizaje y actividad psicomotora en ratas.
Referencias	[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/

Aplicaciones

Métodos	Biomarcadores	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

Información del ensayo clínico

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
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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