Celastrol |
Catalog No.GC15083 |
Celastrol is a proteasome inhibitor with a potent and preferred inhibition of purified 20S proteasome with an IC50 of 2.5 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 34157-83-0
Sample solution is provided at 25 µL, 10mM.
Celastrol is a proteasome inhibitor with a potent and preferred inhibition of purified 20S proteasome with an IC50 of 2.5 μM. Celastrol is also an antioxidant, anti-inflammatory agent, and immunosuppressant that can be used in the study of cancer, autoimmune diseases, asthma, chronic inflammation, and neurodegenerative diseases [1-2].
1-5 μM Celastrol inhibits the chymotrypsin-like activity of the 26S proteasome in human prostate cancer cells, and in PC-3 and LNCaP (androgen receptor-positive) cells, Celastrol leads to the accumulation of ubiquitinating proteins and proteasome substrates (IKB-A, Bax, and p27). And induce apoptosis [1]. Celastrol (0-1 μM) inhibited the proliferation and migration of AGS and YCC-2 cells and increased the number of cells in G1 phase [3]. In addition, Celastrol (0-10 μM) completely inhibits NF-κB activation in TNF-induced lung adenocarcinoma (H1299) cells and embryonic kidney (A293) cells, and Celastrol does not directly affect NF-κB binding to DNA, but inhibits NF-κB activation by inhibiting IKK activation [4].
In PC-3 tumor-bearing nude mice, Celastrol at 1 or 3 mg/kg significantly inhibited tumor growth, with inhibition rates of 65% and 82%, respectively, and a decrease in chymotrypsin-like activity was detected in the tumors of Celastrol-treated mice. (45% and 30% of the control group respectively) [1]. In a mouse model of gastric cancer xenotransplantation, Celastrol (1 or 2 mg/kg) reduced gastric tumor load in a dose-dependent manner, and Celastrol increased phosphorylated AMPK and decreased phosphorylated AKT and mTOR in gastric tumors [3].
References:
[1] Yang H, Chen D, Cui QC, et al. Celastrol, a triterpene extracted from the Chinese "Thunder of God Vine," is a potent proteasome inhibitor and suppresses human prostate cancer growth in nude mice. Cancer Res, 2006, 66(9): 4758-4765.
[2] Salminen A, Lehtonen M, Paimela T, et al. Celastrol: molecular targets of thunder god vine[J]. Biochemical and biophysical research communications, 2010, 394(3): 439-442.
[3] Lee HW, Jang KS, Choi HJ, Jo A, Cheong JH, Chun KH. Celastrol inhibits gastric cancer growth by induction of apoptosis and autophagy. BMB Rep. 2014 Dec;47(12):697-702.
[4] Sethi G, Ahn K S, Pandey M K, et al. Celastrol, a novel triterpene, potentiates TNF-induced apoptosis and suppresses invasion of tumor cells by inhibiting NF-κB–regulated gene products and TAK1-mediated NF-κB activation[J]. Blood, 2007, 109(7): 2727-2735.
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