Celastrol
别名: NSC 70931, Tripterine 中文名称：雷公藤红素
Celastrol是一种有效的蛋白酶抑制剂，有效且优先抑制胰凝乳蛋白酶样的纯化的20S proteasome 的活性，IC50为2.5 μM。Celastrol 可通过ROS/JNK信号传导途径诱导凋亡和自噬。Celastrol 通过激活线粒体凋亡可抑制帕金森氏病的多巴胺能神经元死亡。
Celastrol Chemical Structure
CAS: 34157-83-0
产品质控
批次：
纯度：
99.64%
99.64
Celastrol相关产品
| 相关靶点 | 20S proteasome | 点击展开 |
|---|---|---|
| 相关产品 | MG132 Epoxomicin (BU-4061T) Oprozomib ONX-0914 (PR-957) Delanzomib VR23 Marizomib (Salinosporamide A) PI-1840 | 点击展开 |
| 相关化合物库 | FDA药物库 天然产物库 已知活性药物库-I 蛋白酶抑制剂库 泛素化化合物库 | 点击展开 |
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Celastrol是一种有效的蛋白酶抑制剂，有效且优先抑制胰凝乳蛋白酶样的纯化的20S proteasome 的活性，IC50为2.5 μM。Celastrol 可通过ROS/JNK信号传导途径诱导凋亡和自噬。Celastrol 通过激活线粒体凋亡可抑制帕金森氏病的多巴胺能神经元死亡。 | ||
|---|---|---|---|
| 特性 | Celastrol是一种强效的抗氧化剂和抗炎药。 | ||
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Celastrol在5 μM时，抑制胰凝乳蛋白酶样，PGPH样，胰蛋白酶样的纯化的20S蛋白酶体活性，分别抑制 80％，5％，和<1％。而在10 μM时，抑制这三种蛋白酶体活性分别为~90%，15%，和<1%。Celastrol 作用于PC-3细胞，显著抑制蛋白酶体糜蛋白酶活性，这种作用具有浓度依赖性。2.5 μM到 5 μM Celastrol作用于PC-3细胞，诱导caspase-3 活性提高4.7倍到5.5倍。Celastrol(5 μM) 处理细胞1小时后，蛋白酶体靶蛋白 IκB-α 和 Bax水平提高。Celastrol(2.5 μM)处理LNCaP细胞，抑制40％蛋白酶体，胰凝乳蛋白酶样活性降低，泛素化蛋白积累增加。Celastrol (2.5 μM)作用于Celastrol处理的LNCaP细胞，诱导细胞凋亡，caspase-3活性水平提高（高达3.5倍），且促进PARP裂解和细胞凋亡形态发生。[1]Celastrol (300 nM)抑制LPS诱导的人体单核细胞和巨噬细胞中TNF-α和IL-1β的生产。Celastrol (100 nM)也降低LPS诱导的小胶质细胞中的Ⅱ类MHC分子。Celastrol作用于巨噬细胞，强抑制LPS和IFN-γ诱导的NO产生，IC50为200 nM。Celastrol作用于血管内皮细胞，强抑制TNF-α和IFN-γ诱导的NO产生，IC50为200 nM。[2] Celastrol (2.5 μM) 作用于KBM-5细胞，加强TNF和化疗药物诱导的细胞凋亡，且抑制入侵，这两者同时由NF-κB的激活调节。Celastrol (2.5 μM) 作用于KBM-5细胞，抑制 TNF诱导的参与抗凋亡（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）的基因产物的表达。Celastrol (5 μM)抑制TNF诱导的 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调节的报告基因的表达。[3] Celastrol 抑制RPMI 8226, KATOIII, UM-SCC1, U251MG 和 MDA-MB-231 细胞增殖，IC50分别为0.52 μM, 0.54 μM, 0.76 μM, 0.69 μM 和 0.67 μM。Celastrol(1 μM) 抑制RPMI 8226的生长，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细胞，通过caspase-8激活, Bid 裂解, caspase-9 激活, caspase-3 激活, PARP 裂解,及通过下调抗凋亡蛋白，而诱导细胞凋亡。Celastrol (1 μM) 作用于RPMI-8226 细胞，抑制Akt通路，激活JNK激酶。[4] | |||
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| 激酶实验 | 纯化的20S 蛋白酶体活性抑制实验 | |||
| 纯化的兔20S蛋白酶体(0.1 μg)与40 μM 各种荧光多肽底物在100 μL实验buffer (20 mM Tris-HCl (pH 7.5))中一起温育，其中含不同浓度的Celastrol或DMSO，在37°C下温育2小时，然后测量每种蛋白酶体活性的抑制情况。 | ||||
| 细胞实验 | 细胞系 | RPMI 8226, KATOIII, UM-SCC1, U251MG 和 MDA-MB-231 细胞 | ||
| 浓度 | 5 μM | |||
| 孵育时间 | 2 小时 | |||
| 方法 | 通过MTT摄取法测定Celastrol作用于各种人类肿瘤细胞系的抗增殖作用。5×103细胞与Celastrol按一式三份在96孔板中 37°C下温育。然后每孔加入MTT溶液。在37°C下温育2小时后，加入提取缓冲液（20% SDS, 50%二甲基甲酰胺），细胞在37°C下温育过夜，然后使用Tecan酶标仪在570 nm处测量光密度。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | 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 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Celastrol (3 mg/kg)处理携带PC-3肿瘤的雄性裸鼠，显著抑制肿瘤的生长（抑制高达70％），并提高p27水平和Bax水平。Celastrol(3 mg/kg)处理携带PC-3肿瘤的雄性裸鼠，导致产生更多凋亡肿瘤细胞，并出现各种PARP裂解片段。Celastrol (3 mg/kg) 处理携带C4-2B肿瘤的裸鼠，抑制35％肿瘤，降低蛋白酶体活性，也降低AR蛋白表达。[1] Celastrol (3 mg/kg)处理小鼠，强抑制关节肿胀和和其他反应性关节炎。Celastrol(0.2 mg/kg) 处理大鼠，显著提高记忆，学习,和精神运动活性。[2] | |
|---|---|---|
| 动物实验 | Animal Models | 携带 C4-2B 肿瘤的裸鼠 |
| 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 |
化学信息&溶解度
| 分子量 | 450.61 | 分子式 | C29H38O4 |
| CAS号 | 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 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 90 mg/mL ( (199.72 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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