Celastrol

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Description: Inhibits TNF-α-induced NF-κB activation
Chemical Name: (9β,13α,14β,20α)-3-Hydroxy-9,13-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oic acid
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Reviews
Pathways (1)

Biological Activity for Celastrol

Celastrol is an antioxidant, anti-inflammatory, antitumor and neuroprotective agent. Inhibits lipid peroxidation in mitochondria, TNF-α-induced NFκB activation, peroxidase activity of peroxiredoxin 1 (IC50 = 0.29 μM), and topoisomerase II activity in vitro (IC50 = 7.41 μM). Celastrol treatment inhibits the growth of PC-3 tumors in mice.

Technical Data for Celastrol

M. Wt 450.61
Formula C29H38O4
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 34157-83-0
PubChem ID 122724
InChI Key KQJSQWZMSAGSHN-JJWQIEBTSA-N
Smiles O=C2C(O)=C(C)C1=CC=C([C@](CC[C@]5(C)[C@]([H])4C[C@](C)([C@@](O)=O)CC5)(C)[C@@]4(C)CC3)[C@]3(C)C1=C2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Celastrol

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 45.06 100
ethanol 33.8 75

Preparing Stock Solutions for Celastrol

The following data is based on the product molecular weight 450.61. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.22 mL 11.1 mL 22.19 mL
5 mM 0.44 mL 2.22 mL 4.44 mL
10 mM 0.22 mL 1.11 mL 2.22 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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Product Datasheets for Celastrol

Certificate of Analysis / Product Datasheet
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References for Celastrol

References are publications that support the biological activity of the product.

Nagase et al (2003) Apoptosis induction in HL-60 cells and inhibition of topoisomerase II by triterpene celastrol. Biosci.Biotechnol.Biochem. 67 1883 PMID: 14519971

Sethi et al (2007) 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. Blood 109 2727 PMID: 17110449

Sassa et al (1990) The triterpene celastrol as a very potent inhibitor of lipid peroxidation in mitochondria. Biochem.Biophys.Res.Comms. 172 890 PMID: 2241977

Xu et al (2023) Celastrol suppresses colorectal cancer via covalent targeting peroxiredoxin 1. Signal Transduct.Target Ther. 8 51 PMID: 36732502

Yang et al (2006) 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. 66 4758 PMID: 16651429


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View all NF-κB and IκB Inhibitors

Keywords: Celastrol, Celastrol supplier, inhibitors, inhibits, TNF-α, TNF-alpha-induced, NF-κB, NF-kappaB, NF-kB, activation, Antioxidant, anti-inflammatory, Topoisomerase, II, Nuclear, Factor, Kappa, B, Cytokine, Signaling, Signalling, Transcription, Factors, DNA, Isomerases, tripterine, tripterin, Antioxidants, NF-kB/IkB, 3203, Tocris Bioscience

1 Citation for Celastrol

Citations are publications that use Tocris products. Selected citations for Celastrol include:

Zwicker et al (2015) Interleukin 34: a new modulator of human and experimental inflammatory bowel disease. Clin Sci (Lond) 129 281 PMID: 25896238


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Pathways for Celastrol

NF-κB Signaling Pathway

NF-κB Signaling Pathway

NF-κB signaling plays an important role in inflammation, the innate and adaptive immune response and stress. Dysregulated signaling can occur in inflammatory and autoimmune diseases.