1. Metabolic Enzyme/Protease
    Autophagy
  2. Proteasome
    Autophagy

Celastrol (Synonyms: Tripterin)

Cat. No.: HY-13067 Purity: 99.90%
Handling Instructions

Celastrol is a proteasome inhibitor, potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome (IC50=2.5 μM).

For research use only. We do not sell to patients.
Celastrol Chemical Structure

Celastrol Chemical Structure

CAS No. : 34157-83-0

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 88 In-stock
10 mg USD 80 In-stock
50 mg USD 140 In-stock
100 mg USD 190 In-stock
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Other Forms of Celastrol:

    Celastrol purchased from MCE. Usage Cited in: Mol Biosyst. 2016 Dec 20;13(1):83-91.

    Validation of selected targets of Celastrol identified by competitive proteomics. Western blotting (by using anti-GSTO1 and anti-PDI antibodies) of the pull-down samples upon labeling with IA-yne.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Celastrol is a proteasome inhibitor, potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome (IC50=2.5 μM).

    IC50 & Target

    IC50: 2.5 μM (20S proteasome)[1]

    In Vitro

    Celastrol significantly inhibits the proteasomal chymotrypsin activity in PC-3 cells in a concentration-dependent manner; at 2.5 μM it reaches ~55% inhibition, comparable to its potency to a purified 20S proteasome (IC50=2.5 μM). Furthermore, increased levels of IκB-α, Bax, and p27 are observed, three well known target proteins of the proteasome in PC-3 cells treated with Celastrol[1].

    In Vivo

    Treatment of PC-3 tumor-bearing nude mice with Celastrol (1-3 mg/kg/d, i.p., 1-31 days) results in significant inhibition (65-93%) of the tumor growth[1]. Following treatment with 3 and 6 mg/kg Celastrol, the levels of malondialdehyde (MDA) are significantly decreased by 35.2 and 36.7% (P<0.05), respectively. Treatment with 3 and 6 mg/kg Celastrol markedly restores the GSH level (P<0.05) to almost normal levels[2].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.2192 mL 11.0961 mL 22.1921 mL
    5 mM 0.4438 mL 2.2192 mL 4.4384 mL
    10 mM 0.2219 mL 1.1096 mL 2.2192 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [1]

    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 or Oridonin at different concentrations or in the solvent DMSO for 2 hours at 37°C, followed by measurement of inhibition of each proteasomal activity[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    Celastrol is dissolved in DMSO (50 mM) and stored, and then diluted with appropriate media before use[1].

    Prostate cancer cells (5,000-8,000) are plated in each well of a 96-well plate and then treated with either DMSO, Celastrol, or Oridonin at different concentrations for 12 to 16 hours, followed by an additional 2-hour incubation with Z-Gly-Gly-Leu-AMC (at 40 μM). After that, the proteasome activity is measured using the whole plate[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1][2]

    Celastrol is prepared in 10% DMSO, 70% Cremophor/ethanol (3:1), and 20% PBS (Mice)[1].
    Celastrol is prepared in distilled water (Rats)[2].

    Mice[1]
    Male nude immunodeficient mice NCRNU-M, aged 5 weeks, are used. On day 0, human prostate cancer PC-3 or C4-2B cells (5-10×106) suspended in 0.1 mL of serum-free RPMI 1640 are inoculated s.c. in the right flank of each mouse (four mice per group). For the first experiment using PC-3 cells, on day 14 after inoculation, the animals started daily i.p. injection with either 50 to 100 μL of a vehicle [10% DMSO, 70% Cremophor/ethanol (3:1), and 20% PBS], and 1.0 or 3.0 mg/kg of Celastrol. Tumor sizes are measured daily using calipers and their volumes are calculated using a standard formula: width2×length/2. Body weight is measured weekly. To study whether the proteasome is inhibited in an early phase of the experiment, after 3 days of treatment, one control and one 3.0 mg/kg Celastrol-treated mouse is sacrificed. The rest are sacrificed after 16 days of treatment when control tumors reach 1,400 mm3. For the second PC-3 tumor experiment, 12 days after inoculation, mice are randomly divided into three groups and treated with either control, Celastrol, or Oridonin at 1.5 mg/kg daily for the duration of the study (31 days). In another experiment, to study the effects of Celastrol on AR expression, nude mice bearing C4-2B tumors receive daily i.p. injection of the vehicle or 3.0 mg/kg Celastrol.
    Rats[2]
    Male Sprague-Dawley (SD) rats (n=90, 6 weeks old), weighing 161±9 g, are randomly divided into the control (NC) and the high energy diet (HED) groups. In the control group, the animals receive a standard chow diet, while the rats in the HED group are fed with an additional high energy emulsion. After 8 weeks on their respective diets, Streptozotocin (STZ; 45 mg/kg) dissolved in 0.1 mol/l citrate buffer (pH 4.5) is injected into the caudal vein of the rats in the HED group to establish a model of T2DM, while the rats in the control group are injected with sodium citrate buffer. The rats with blood glucose levels ≥16.7 mM at 7 days after the STZ injection are selected as the model of diabetes. On average, 80% of the rats injected with STZ met these criteria. At 1 week following the injection of STZ, the rats with successfully-induced diabetes are randomly divided into the diabetes model (DM) group, the Celastrol low-dose group (1 mg/kg/day), the Celastrol middle-dose group (3 mg/kg/day) and the Celastrol high-dose group (6 mg/kg/day) (n=15 rats per group). The rats in the treatment groups are administered Celastrol by gavage, whereas the rats in the NC and DM groups are administered an equal amount of distilled water (2 mL). Following 8 weeks of the respective treatments, rats are anesthetized with an intraperitoneal injection of sodium pentobarbital (30 mg/kg body weight) and tissue samples are collected for analysis. The paravertebral muscle is excised from the rat bodies, and is cut perpendicularly along the longitudinal axis and fixed in phosphate-buffered 20% formaldehyde. Histological paraffin-embedded sections (5 µm) are then prepared for H&E staining. The sections of paravertebral muscle are snap-frozen in liquid nitrogen and stored at −80°C until further analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    450.61

    Formula

    C₂₉H₃₈O₄

    CAS No.

    34157-83-0

    SMILES

    OC1=C(C2=CC=C3[[email protected]](C)([[email protected]]4(CC[[email protected]]3(C2=CC1=O)C)C)CC[[email protected]@]5(C)CC[[email protected]@](C(O)=O)(C[[email protected]]54[H])C)C

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.90%

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    Inquiry Information

    Product Name:
    Celastrol
    Cat. No.:
    HY-13067
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