Celastrol (NSC 70931) - Moligand™, 10mM in DMSO , Inhibitor of regulator of G-protein signaling 17, CAS No.34157-83-0, Inhibitor of regulator of G-protein signaling 17

CAS: 34157-83-0 Cat. No.: C408328 Peso molecular: 450.61 Número EC: 636-472-5

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

Tripterine | (2R,4aS,6aS,12bR,14aS,14bR)-10-hydroxy-2,4a,6a,9,12b,14a-hexamethyl-11-oxo-1,2,3,4,4a,5,6,6a,11,12b,13,14,14a,14b-tetradecahydropicene-2-carboxylic acid

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Celastrol (NSC 70931, Tripterine) is a potentproteasomeinhibitor for the chymotrypsin-like activity of a purified 20S proteasome withIC50of 2.5 μM. Celastrol inducesapoptosisandautophagyvia the ROS/JNK signaling pathway. Celastrol inhibits dopaminergic ne
In vitro

Celastrol at 5 μM inhibits the chymotrypsin-like, PGPH-like, and trypsin-like activities of the purified 20S proteasome by 80%, 5%, and <1%, respectively, whereas at 10 μM, it inhibits these three proteasomal activities by ∼90%, 15%, and <1%, respectively. Celastrol significantly inhibits the proteasomal chymotrypsin activity in PC-3 cells in a concentration-dependent manner. Celastrol at 2.5 μM to 5 μM induces caspase-3 activity by 4.7-fold to 5.5-fold in PC-3 cells. Celastrol (5 μM) treated cells, the levels of the proteasome target proteins, IκB-α and Bax, are increased after 1 hour and further increased to its peak for 4 hours to 12 hours. Celastrol (2.5 μM) treatment induces proteasome inhibition by 40%, as shown by the decreased levels of chymotrypsin-like activity and increased accumulation of ubiquitinated proteins in LNCaP cells. Celastrol (2.5 μM) induces apoptosis in the Celastrol-treated LNCaP cells, as shown by increased levels of caspase-3 activity (up to 3.5-fold), PARP cleavage, and apoptotic morphology. Celastrol (300 nM) is found to suppress LPS-induced production of TNF-alpha and IL-1beta by human monocytes and macrophages. Celastrol (100 nM) also decreases LPS-induced expression of class II MHC molecules by microglia. Celastrol strongly inhibits LPS and IFN-y-induced NO production with IC50 of 200 nM in macrophage lineage cells. Celastrol strongly inhibits TNF-α and IFN-γ-induced NO production with IC50 of 200 nM in endothelial cells. Celastrol (2.5 μM) potentiates the apoptosis induced by TNF and chemotherapeutic agents and inhibits invasion, both regulated by NF-kappaB activation, in KBM-5 cells. Celastrol (2.5 μM) suppresses the expression of TNF induced the expression of gene products involved in antiapoptosis (IAP1, IAP2, Bcl-2, Bcl-XL, c-FLIP, and survivin), proliferation (cyclin D1 and COX-2), invasion (MMP-9), and angiogenesis (VEGF) in KBM-5 cells. Celastrol (5 μM) is found to inhibit the TNF-induced activation of IkappaBalpha kinase, IkappaBalpha phosphorylation, IkappaBalpha degradation, p65 nuclear translocation and phosphorylation, and NF-kappaB-mediated reporter gene expression. Celastrol inhibits proliferating of RPMI 8226, KATOIII, UM-SCC1, U251MG and MDA-MB-231 cells with IC50 of 0.52 μM, 0.54 μM, 0.76 μM, 0.69 μM and 0.67 μM, respectively. Celastrol (1 μM) inhibits growth of RPMI 8226 with a decrease in the levels of cyclin D1 and cyclin E, but concomitant increase in the levels of p21 and p27. Celastrol induces apoptosis in RPMI-8226 cells indicated by the activation of caspase-8, bid cleavage, caspase-9 activation, caspase-3 activation, PARP cleavage and through the down regulation of anti-apoptototic proteins. Celastrol (1 μM) suppresses Akt pathway and activates JNK kinase in RPMI-8226 cells.

In vivo

Celastrol (3 mg/kg) results in significant inhibition (up to 70%) of tumor growth in male nude mice bearing PC-3 tumors, associated with increased p27 levels and Bax level. Celastrol (3 mg/kg) results more apoptotic tumor cells with the appearance of various PARP cleavage fragments in tumor of male nude mice bearing PC-3 tumors. Celastrol (3 mg/kg) causes 35% of tumor inhibition, associated with decreased proteasome activity and decreased expression of AR protein in nude mice bearing C4-2B tumors. Celastrol (3 mg/kg) is found to suppress strongly joint swelling and other manifestations of adjuvant arthritis in mice. Celastrol (0.2 mg/kg) significantly improves the performance in memory, learning and psychomotor activity tests in rats.
Cell Data

cell lines：

Concentrations：~5 μM

Incubation Time：2 hours

Powder Purity:≥98%

Specifications

Sinónimos

Tripterine | (2R, 4aS, 6aS, 12bR, 14aS, 14bR)-10-hydroxy-2, 4a, 6a, 9, 12b, 14a-hexamethyl-11-oxo-1, 2, 3, 4, 4a, 5, 6, 6a, 11, 12b, 13, 14, 14a, 14b-tetradecahydropicene-2-carboxylic acid

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Celastrol (NSC 70931, Tripterine) is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. Celastrol induces apoptosis and autophagy via the ROS/JNK signaling pathway. Celastrol inhibits dopamin

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Inhibitor of regulator of G-protein signaling 17

Nombres e identificadores

• Isómeros SMILES: CC1=C(C(=O)C=C2C1=CC=C3[C@]2(CC[C@@]4([C@@]3(CC[C@@]5([C@H]4C[C@](CC5)(C)C(=O)O)C)C)C)C)O
• WGK Alemania: 2
• CAS alternativo: 34157-83-0
• Número NSC: 70931
• Número ONU: 2811
• Términos de entrada MeSH: 3-hydroxy-24-nor-2-oxo-1(10),3,5,7-friedelatetraen-29-oic acid;celastrol;tripterin;tripterine
• Peso molecular: 450.61
• Reaxy-Rn: 5780870
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=5780870&ln=

Objetivos asociados (humanos)

HIF1A Tchem Hypoxia-inducible factor 1-alpha (1 Activities)

Discover Target: HIF1A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TERT Tchem Telomerase reverse transcriptase (1 Activities)

Discover Target: TERT

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro Water: 28 mg/mL (199.18 mM); DMSO: Insoluble; Ethanol: Insoluble
• Rotación específica [α]: -122.7° (C=0.1,CHCl3)
• Punto de fusión (°C): 203°C(lit.)

Referencias

1. Min Wei, Yi Liu, Dongsheng Li, Xingdong Wang, Xiaodong Wang, Yuping Li, Zhengcun Yan, Hengzhu Zhang.  (2024)  Celastrol alleviates secondary brain injury following intracerebral haemorrhage by inhibiting neuronal ferroptosis and blocking blood-brain barrier disruption.  IBRO Neuroscience Reports,      [PMID:39220228] [10.1016/j.ibneur.2024.08.003]

2. Wanfen Liao, Aiwen Dong, Fatima Hafeez, Qinyong Ye, En Huang.  (2025)  Celastrol protected the MPTP-injected mice Parkinson's disease model via redox regulation of CDC37.  PHYTOMEDICINE,      [PMID:40652801] [10.1016/j.phymed.2025.157067]

3. Ping Sheng, Chao Bu, Tanyue Hui, Lili Zhou, Hao Chen, Guoliang Zhou.  (2023)  Polydopamine-activated celastrol carbon dots for synergistic chemotherapy-photothermal therapy of tumors.  International Journal of Pharmaceutics-X,      [PMID:38033396] [10.1016/j.ijpx.2023.100218]

4. Jiwen Fan, Meng Ren, Weiwei Chen, Haodong Wang, Yuquan He.  (2023)  Celastrol relieves myocardial infarction-induced cardiac fibrosis by inhibiting NLRP3 inflammasomes in rats.  INTERNATIONAL IMMUNOPHARMACOLOGY,      [PMID:37343368] [10.1016/j.intimp.2023.110511]

5. Xiaoli Li, Guangbei Zhu, Xintong Yao, Ning Wang, Ronghui Hu, Qingxin Kong, Duanfang Zhou, Liangyuan Long, Jiali Cai, Weiying Zhou.  (2022)  Celastrol induces ubiquitin-dependent degradation of mTOR in breast cancer cells.  OncoTargets and Therapy,      [PMID:30588010] [10.2147/OTT.S187315]

6. Qiang Chen, Chunjing Guo, Zhongxin Liu, Min Cao, Wenxin Wang, Dandan Zhang, Hongxu Geng, Ningning Diao, Daquan Chen.  (2022)  Multifunctional nanoparticles with anti-inflammatory effect for improving metabolic syndromes.  JOURNAL OF DRUG TARGETING,      [PMID:36315421] [10.1080/1061186X.2022.2142595]

7. Bo Yu, Yiping Shen, Xuejie Zhang, Lijuan Ding, Zheng Meng, Xiaotong Wang, Meihua Han, Yifei Guo, Xiangtao Wang.  (2022)  Poly(methacrylate citric acid) as a Dual Functional Carrier for Tumor Therapy.  Pharmaceutics,  14  (9): (1765).  [PMID:36145512] [10.3390/pharmaceutics14091765]

8. Lin Jingpan, Gao Lu, Lin Yanke, Wang Shuai, Yang Zemin, Ren Shujing, Chen Min, Wu Baojian.  (2021)  Pharmacokinetics-Based Chronoefficacy of Semen Strychni and Tripterygium Glycoside Tablet Against Rheumatoid Arthritis.  Frontiers in Pharmacology,      [PMID:34108880] [10.3389/fphar.2021.673263]

9. Niu Weina, Wang Jianguo, Wang Qinyao, Shen Jianjun.  (2020)  Celastrol Loaded Nanoparticles With ROS-Response and ROS-Inducer for the Treatment of Ovarian Cancer.  Frontiers in Chemistry,      [PMID:33195064] [10.3389/fchem.2020.574614]

10. Zhao Huan, Tong Yongbin, Lu Danyi, Wu Baojian.  (2020)  Circadian clock regulates hepatotoxicity of Tripterygium wilfordii through modulation of metabolism.  JOURNAL OF PHARMACY AND PHARMACOLOGY,  72  (12): (1854-1864).  [PMID:32478421] [10.1111/jphp.13299]

11. Jian Lu, Daozhi Liu, Xiaojing Zhou, Ang Chen, Zhenran Jiang, Xiyun Ye, Mingyao Liu, Xin Wang.  (2017)  Plant natural product plumbagin presents potent inhibitory effect on human cytochrome P450 2J2 enzyme.  PHYTOMEDICINE,      [PMID:29433675] [10.1016/j.phymed.2017.12.026]

12. Yang Hongbin, Liu Chang, Jiang Jie, Wang Yuena, Zhang Xiaoyu.  (2017)  Celastrol Attenuates Multiple Sclerosis and Optic Neuritis in an Experimental Autoimmune Encephalomyelitis Model.  Frontiers in Pharmacology,      [PMID:28239352] [10.3389/fphar.2017.00044]

13. Hu Yingying, Nan Yan, Lin Hongzhou, Zhao Qianlei, Chen Tingting, Tao Xiaoyue, Ding Bingqing, Lu Liying, Chen Shangqin, Zhu Jianghu, Guo Xiaoling, Lin Zhenlang.  (2024)  Celastrol ameliorates hypoxic-ischemic brain injury in neonatal rats by reducing oxidative stress and inflammation.  PEDIATRIC RESEARCH,      [PMID:38763946] [10.1038/s41390-024-03246-9]

14. Yunyan Chen, Ziwei Zhang, Zhilei Qian, Rui Ma, Minna Luan, Yu Sun.  (2024)  Sequentially Released Liposomes Enhance Anti-Liver Cancer Efficacy of Tetrandrine and Celastrol-Loaded Coix Seed Oil.  International Journal of Nanomedicine,      [PMID:38288265] [10.2147/IJN.S446895]

15. Yunpeng Qi, Renping Wang, Liang Zhao, Lei Lv, Fan Zhou, Tian Zhang, Feng Lu, Hongli Yan, Gengli Duan.  (2018)  Celastrol Suppresses Tryptophan Catabolism in Human Colon Cancer Cells as Revealed by Metabolic Profiling and Targeted Metabolite Analysis.  BIOLOGICAL & PHARMACEUTICAL BULLETIN,  41  (8): (1243-1250).  [PMID:30068874] [10.1248/bpb.b18-00171]

16. Simeng Xiao, Yun Zhao, Zhiguo Chen, Yangkun Xiong, Dingmei Zhang, Gang Zhou, Cong Zhang.  (2025)  Celastrol delays the progression of hepatocellular carcinoma by suppressing SLC1A5-mediated glutamine dependence.  TOXICOLOGY AND APPLIED PHARMACOLOGY,      [PMID:41401867] [10.1016/j.taap.2025.117690]

17. Chen Yigang, Ji Xiang, Zhang Ziyue, Zhu Zihao, Zhou Yuming, Su Chang, Lin Yang-Chi-Dung, Huang Hsi-Yuan, Wei Kangping, Lai Yi, Chen Ke, Lin Xingqiao, Zhang Yangyi, Fu Jiehui, Huang Yixian, Cui Shidong, Yen Shih-Chung, Zhang Tao, Warshel Arieh, Huang Hsien-Da.  (2025)  Semi-inductive dataset construction and framework optimization for practical drug target interaction prediction with ScopeDTI.  Nature Communications,  16  (1): (11509).  [PMID:41390462] [10.1038/s41467-025-66311-9]

18. Yangwang Jin, Fei Qin, Ranxing Yang, Wenzhuo Fang, Kaile Zhang, Meng Liu, Ming Yang, Ying Wang, Qiang Fu.  (2026)  Dynamic microenvironment-regulated hydrogels releasing celastrol lead to urethral scarless repair.  Materials Today Bio,      [PMID:41737466] [10.1016/j.mtbio.2026.102917]

19. Jinrun Chen, Yuqin Wu, Bofei Xu, Jiabei Hou, Yijing Li, Yuhan Hu, Yutuo Zhu, Wenqiao Zhang, Shuqi Feng, Huanting Jin, Yuchen Cheng, Yuanyuan Jin, Jianhong Zhou, Xingyi Li.  (2026)  Oral Celastrol Nanomedicine Targeting Intestinal Antigen-Presenting Cells to Effectively Mitigate Autoimmune Uveitis via Gut-Retina Axis.  Advanced Science,      [PMID:41632039] [10.1002/advs.202519503]

20. Huan Liu, Liying Liang, Minggang Wang, Qinfeng Huang, Yu Pan, Xiaojie Wei, Wenchao Zhang.  (2026)  Establishment of a Novel Monoclonal Antibody Based icELISA Method to Determine the Total Content of Ursolic and Oleanolic Acids in Fruits.  JOURNAL OF FOOD COMPOSITION AND ANALYSIS,      [PMID:] [10.1016/j.jfca.2026.109072]

21. Li Zhu, Yue Zheng, Mengjuan Yu, Shan Yu, Yiyun Luo, Ravin Narain, Kaihui Nan, Yangjun Chen.  (2026)  Celastrol-loaded micelles with dual-mucoadhesive strategy for efficient suppression of corneal neovascularization.  CHEMICAL ENGINEERING JOURNAL,      [PMID:] [10.1016/j.cej.2026.174711]