Celastrol

• CAT Number: I003238
• CAS Number: 34157-83-0
• Molecular Formula: C29H38O4
• Molecular Weight: 450.61
• Purity: ≥95%
• Target: Proteasome
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IUPAC Name: (2R,4aS,6aR,6aS,14aS,14bR)-10-hydroxy-2,4a,6a,6a,9,14a-hexamethyl-11-oxo-1,3,4,5,6,13,14,14b-octahydropicene-2-carboxylic acid
• InChI: InChI=1S/C29H38O4/c1-17-18-7-8-21-27(4,19(18)15-20(30)23(17)31)12-14-29(6)22-16-26(3,24(32)33)10-9-25(22,2)11-13-28(21,29)5/h7-8,15,22,31H,9-14,16H2,1-6H3,(H,32,33)/t22-,25-,26-,27+,28-,29+/m1/s1
• InChIKey: KQJSQWZMSAGSHN-JJWQIEBTSA-N
• SMILES: CC1=C(C(=O)C=C2C1=CC=C3C2(CCC4(C3(CCC5(C4CC(CC5)(C)C(=O)O)C)C)C)C)O

Celastrol(CAT: I003238), also known as tripterin, is a natural compound derived from the root bark of the traditional Chinese medicinal plant Tripterygium wilfordii. It has been found to possess potent antioxidant and anti-inflammatory properties. Additionally, celastrol has been identified as a novel inhibitor of heat shock protein 90 (HSP90), a chaperone protein involved in the stabilization and function of various client proteins, including oncogenic signaling molecules. The inhibition of HSP90 by celastrol can disrupt multiple signaling pathways involved in cancer cell survival and proliferation, making it a potential candidate for cancer therapy.

Overview of Clinical Research

Celastrol(Tripterin) is a DNA topoisomerase I inhibitor and a protein tyrosine kinase inhibitor. 

Reference

1:Celastrol inhibits chondrosarcoma proliferation, migration and invasion through suppression CIP2A/c-MYC signaling pathway. Wu J, Ding M, Mao N, Wu Y, Wang C, Yuan J, Miao X, Li J, Shi Z.J Pharmacol Sci. 2017 Apr 14. pii: S1347-8613(17)30057-9. doi: 10.1016/j.jphs.2016.12.007. [Epub ahead of print] PMID: 28522217
2:AlCl₃·6H₂O-Catalyzed Friedel-Crafts Alkylation of Indoles by the para-Quinone Methide Moiety of Celastrol. Zhu Y, Chen Z, Huang Z, Yan S, Li Z, Zhou H, Zhang X, Su Y, Zeng Z.Molecules. 2017 May 16;22(5). pii: E742. doi: 10.3390/molecules22050742. PMID: 28509859 Free Article
3:Cytotoxic effect of celastrol alone or in combination with paclitaxel on anaplastic thyroid carcinoma cells. Kim SH, Kang JG, Kim CS, Ihm SH, Choi MG, Yoo HJ, Lee SJ.Tumour Biol. 2017 May;39(5):1010428317698369. doi: 10.1177/1010428317698369. PMID: 28459364
4:Celastrol reduces IL-1β induced matrix catabolism, oxidative stress and inflammation in human nucleus pulposus cells and attenuates rat intervertebral disc degeneration in vivo. Chen J, Xuan J, Gu YT, Shi KS, Xie JJ, Chen JX, Zheng ZM, Chen Y, Chen XB, Wu YS, Zhang XL, Wang XY.Biomed Pharmacother. 2017 Apr 27;91:208-219. doi: 10.1016/j.biopha.2017.04.093. [Epub ahead of print] PMID: 28458159
5:Repression of acetaminophen-induced hepatotoxicity by a combination of celastrol and brilliant blue G. Abdelaziz HA, Shaker ME, Hamed MF, Gameil NM.Toxicol Lett. 2017 Apr 21;275:6-18. doi: 10.1016/j.toxlet.2017.04.012. [Epub ahead of print] PMID: 28435131
6:Celastrol protects TGF-β1-induced endothelial-mesenchymal transition. Gong F, Zhao F, Gan XD.J Huazhong Univ Sci Technolog Med Sci. 2017 Apr;37(2):185-190. doi: 10.1007/s11596-017-1713-0. Epub 2017 Apr 11. PMID: 28397045
7:Autophagy induction by celastrol augments protection against bleomycin-induced experimental pulmonary fibrosis in rats: Role of adaptor protein p62/ SQSTM1. Divya T, Sureshkumar A, Sudhandiran G.Pulm Pharmacol Ther. 2017 Apr 4. pii: S1094-5539(17)30034-2. doi: 10.1016/j.pupt.2017.04.003. [Epub ahead of print] PMID: 28389259
8:Celastrol-Induced Nur77 Interaction with TRAF2 Alleviates Inflammation by Promoting Mitochondrial Ubiquitination and Autophagy. Hu M, Luo Q, Alitongbieke G, Chong S, Xu C, Xie L, Chen X, Zhang D, Zhou Y, Wang Z, Ye X, Cai L, Zhang F, Chen H, Jiang F, Fang H, Yang S, Liu J, Diaz-Meco MT, Su Y, Zhou H, Moscat J, Lin X, Zhang XK.Mol Cell. 2017 Apr 6;66(1):141-153.e6. doi: 10.1016/j.molcel.2017.03.008. PMID: 28388439
9:Celastrol, an active constituent of the TCM plant Tripterygium wilfordii Hook.f., inhibits prostate cancer bone metastasis. Kuchta K, Xiang Y, Huang S, Tang Y, Peng X, Wang X, Zhu Y, Li J, Xu J, Lin Z, Pan T.Prostate Cancer Prostatic Dis. 2017 Jun;20(2):250. doi: 10.1038/pcan.2017.11. Epub 2017 Mar 28. No abstract available. PMID: 28349980
10:Celastrol Attenuates Multiple Sclerosis and Optic Neuritis in an Experimental Autoimmune Encephalomyelitis Model. Yang H, Liu C, Jiang J, Wang Y, Zhang X.Front Pharmacol. 2017 Feb 10;8:44. doi: 10.3389/fphar.2017.00044. eCollection 2017. PMID: 28239352 Free PMC Article