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Celastrol

別名: NSC 70931, Tripterine 中文名稱：雷公藤紅素

Celastrol是一種有效的蛋白酶抑制劑，有效且優(yōu)先抑制胰凝乳蛋白酶樣的純化的20S proteasome 的活性，IC50為2.5 μM。Celastrol 可通過ROS/JNK信號傳導途徑誘導凋亡和自噬。Celastrol 通過激活線粒體凋亡可抑制帕金森氏病的多巴胺能神經元死亡。

Celastrol Chemical Structure

Celastrol Chemical Structure

CAS: 34157-83-0

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1040.77 現(xiàn)貨
10mg 898.79 現(xiàn)貨
50mg 2449.18 現(xiàn)貨
1g 20229.3 現(xiàn)貨
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Celastrol相關產品

相關信號通路圖

Proteasome Signaling Pathways

Proteasome信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
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
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
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
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
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
HeLa Cytotoxicity assay 72 hrs Cytotoxicity against human HeLa cells after 72 hrs by MTS assay, CC50 = 3 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
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 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
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
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
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
RAW264 Function assay 24 hrs Inhibition of LPS-induced NO production in mouse RAW264 cells after 24 hrs 21393004
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 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
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
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
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
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
LNCAP Antitumor assay Antitumor activity against human LNCAP cells, IC50 = 2.5 μM. 20627556
HeLa Function assay Inhibition of NF-kappaB activity in human HeLa cells by SEAP reporter assay, IC50 = 0.15 μM. 20469887
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
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
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
RPMI8226 Growth inhibition assay Growth inhibition of human RPMI8226 cells, IC50 = 3 μM. 18164197
PC12 Cytoprotective assay Cytoprotective activity against t-BPH-induced cell damage in rat PC12 cells assessed as cell viability, IC50 = 3.15 μM. 20627556
293T Cytotoxicity assay Cytotoxicity against human 293T cells assessed as cell viability by dual-luciferase reporter assay, IC50 = 0.67 μM. 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 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
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
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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生物活性

產品描述 Celastrol是一種有效的蛋白酶抑制劑，有效且優(yōu)先抑制胰凝乳蛋白酶樣的純化的20S proteasome 的活性，IC50為2.5 μM。Celastrol 可通過ROS/JNK信號傳導途徑誘導凋亡和自噬。Celastrol 通過激活線粒體凋亡可抑制帕金森氏病的多巴胺能神經元死亡。
特性 Celastrol是一種強效的抗氧化劑和抗炎藥。
靶點
20S proteasome [1]
(Cell-free assay)
2.5 μM
體外研究(In Vitro)
體外研究活性 Celastrol在5 μM時，抑制胰凝乳蛋白酶樣，PGPH樣，胰蛋白酶樣的純化的20S蛋白酶體活性，分別抑制 80％，5％，和<1％。而在10 μM時，抑制這三種蛋白酶體活性分別為~90%，15%，和<1%。Celastrol 作用于PC-3細胞，顯著抑制蛋白酶體糜蛋白酶活性，這種作用具有濃度依賴性。2.5 μM到 5 μM Celastrol作用于PC-3細胞，誘導caspase-3 活性提高4.7倍到5.5倍。Celastrol(5 μM) 處理細胞1小時后，蛋白酶體靶蛋白 IκB-α 和 Bax水平提高。Celastrol(2.5 μM)處理LNCaP細胞，抑制40％蛋白酶體，胰凝乳蛋白酶樣活性降低，泛素化蛋白積累增加。Celastrol (2.5 μM)作用于Celastrol處理的LNCaP細胞，誘導細胞凋亡，caspase-3活性水平提高（高達3.5倍），且促進PARP裂解和細胞凋亡形態(tài)發(fā)生。[1]Celastrol (300 nM)抑制LPS誘導的人體單核細胞和巨噬細胞中TNF-α和IL-1β的生產。Celastrol (100 nM)也降低LPS誘導的小膠質細胞中的Ⅱ類MHC分子。Celastrol作用于巨噬細胞，強抑制LPS和IFN-γ誘導的NO產生，IC50為200 nM。Celastrol作用于血管內皮細胞，強抑制TNF-α和IFN-γ誘導的NO產生，IC50為200 nM。[2] Celastrol (2.5 μM) 作用于KBM-5細胞，加強TNF和化療藥物誘導的細胞凋亡，且抑制入侵，這兩者同時由NF-κB的激活調節(jié)。Celastrol (2.5 μM) 作用于KBM-5細胞，抑制 TNF誘導的參與抗凋亡（IAP1, IAP2, Bcl-2, Bcl-XL, c-FLIP, 和 survivin），增殖（cyclin D1 和 COX-2），入侵（MMP-9），和血管生成（VEGF）的基因產物的表達。Celastrol (5 μM)抑制TNF誘導的 IkappaBα激酶的激活，IkappaBα的磷酸化，IkappaBα的降解，p65核易位和磷酸化，及NF-κB調節(jié)的報告基因的表達。[3] Celastrol 抑制RPMI 8226, KATOIII, UM-SCC1, U251MG 和 MDA-MB-231 細胞增殖，IC50分別為0.52 μM, 0.54 μM, 0.76 μM, 0.69 μM 和 0.67 μM。Celastrol(1 μM) 抑制RPMI 8226的生長，降低cyclin D1和cyclin E的水平，但增加p21和p27的水平。Celastrol 作用于RPMI-8226細胞，通過caspase-8激活, Bid 裂解, caspase-9 激活, caspase-3 激活, PARP 裂解,及通過下調抗凋亡蛋白，而誘導細胞凋亡。Celastrol (1 μM) 作用于RPMI-8226 細胞，抑制Akt通路，激活JNK激酶。[4]
激酶實驗 純化的20S 蛋白酶體活性抑制實驗
純化的兔20S蛋白酶體(0.1 μg)與40 μM 各種熒光多肽底物在100 μL實驗buffer (20 mM Tris-HCl (pH 7.5))中一起溫育，其中含不同濃度的Celastrol或DMSO，在37°C下溫育2小時，然后測量每種蛋白酶體活性的抑制情況。
細胞實驗 細胞系 RPMI 8226, KATOIII, UM-SCC1, U251MG 和 MDA-MB-231 細胞
濃度 5 μM
孵育時間 2 小時
方法 通過MTT攝取法測定Celastrol作用于各種人類腫瘤細胞系的抗增殖作用。5×103細胞與Celastrol按一式三份在96孔板中 37°C下溫育。然后每孔加入MTT溶液。在37°C下溫育2小時后，加入提取緩沖液（20% SDS, 50%二甲基甲酰胺），細胞在37°C下溫育過夜，然后使用Tecan酶標儀在570 nm處測量光密度。
實驗圖片 檢測方法 檢測指標 實驗圖片 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
體內研究(In Vivo)
體內研究活性 Celastrol (3 mg/kg)處理攜帶PC-3腫瘤的雄性裸鼠，顯著抑制腫瘤的生長（抑制高達70％），并提高p27水平和Bax水平。Celastrol(3 mg/kg)處理攜帶PC-3腫瘤的雄性裸鼠，導致產生更多凋亡腫瘤細胞，并出現(xiàn)各種PARP裂解片段。Celastrol (3 mg/kg) 處理攜帶C4-2B腫瘤的裸鼠，抑制35％腫瘤，降低蛋白酶體活性，也降低AR蛋白表達。[1] Celastrol (3 mg/kg)處理小鼠，強抑制關節(jié)腫脹和和其他反應性關節(jié)炎。Celastrol(0.2 mg/kg) 處理大鼠，顯著提高記憶，學習,和精神運動活性。[2]
動物實驗 Animal Models 攜帶 C4-2B 腫瘤的裸鼠
Dosages 3 mg/kg
Administration 腹腔注射
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05494112 Recruiting
Safety
Legend Labz Inc.
 May 25 2022 Not Applicable
NCT05413226 Recruiting
Safety Issues
Legend Labz Inc.
 September 28 2021 Not Applicable

化學信息&溶解度

分子量 450.61 分子式

C29H38O4
CAS號 34157-83-0 SDF Download Celastrol SDF
Smiles CC1=C(C(=O)C=C2C1=CC=C3C2(CCC4(C3(CCC5(C4CC(CC5)(C)C(=O)O)C)C)C)C)O
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 90 mg/mL ( (199.72 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內配方計算器

實驗計算

摩爾濃度計算器

質量 濃度 體積 分子量

動物體內配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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