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Biological Description

Description: Celastrol is an effective proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome(IC50=2.5 μM) with antioxidant and anti-inflammatory activity.

Targets&IC50: 20S proteasome:2.5 μM

Kinase Assay: Inhibition of purified 20S proteasome activity: A purified rabbit 20S proteasome (0.1 μg) is incubated with 40 μM of various fluorogenic peptide substrates in 100 μL assay buffer (20 mM Tris-HCl (pH 7.5)), in the presence of Celastrol at different concentrations or in the solvent DMSO for 2 hours at 37 ℃, followed by measurement of inhibition of each proteasomal activity.

Cell Research: The anti-proliferative effect of celastrol on various human tumor cell lines is determined by the MTT uptake method. Briefly, 5×103 cells are incubated with Celastrol in triplicate in a 96-well plate at 37 ℃. MTT solution is then added to each well. After a 2 hours incubation at 37 ℃, extraction buffer (20% SDS, 50% dimethylformamide) is added, cells are incubated overnight at 37 ℃, and the optical density is then measured at 570 nm using a Tecan plate reader.(Only for Reference)

Chemical Properties

Molecular Weight: 450.619

Formula: C29H38O4

CAS No.: 34157-83-0

Storage & Solubility Information

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 45.1 mg/mL (100 mM)

Ethanol: 33.8 mg/mL (75 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Catalog #: T3028

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References and Literature

1. Yang H, et al. Cancer Res, 2006, 66(9), 4758-4765.

2. Allison AC, et al. Prog Neuropsychopharmacol Biol Psychiatry, 2001, 25(7), 1341-1357.

3. Sethi G, et al. Blood, 2007, 109(7), 2727-2735.

4. Kannaiyan R, et al. Apoptosis, 2011, 16(10), 1028-1041.

5. Liu Q, Yue Y, Wang S, et al. Celastrol Attenuates the Remodeling of Pulmonary Vascular and Right Ventricular in Monocrotaline-Induced Pulmonary Arterial Hypertension in Rats[J]. 2021

6. Jiang X, Chen S, Zhang Q, et al. Celastrol is a novel selective agonist of cannabinoid receptor 2 with anti-inflammatory and anti-fibrotic activity in a mouse model of systemic sclerosis[J]. Phytomedicine. 2019: 153160.