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    CELASTROL
    CELASTROL

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0693
    CAS #: 34157-83-0Purity ≥98%

    Description: Celastrol (also called tripterine) is a naturally occurring pentacyclic nortriterpen quinone and a remedial ingredient found in the root extracts of Tripterygium Wilfordi (Thunder of God vine) and Celastrus Regelii. It acts as a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome (IC50 = 2.5 μM), and also as an NR4A1 agonist with potential anti-inflammatory and anticancer activity.

    Related CAS #: 193957-88-9 (dihydrocelastrol)    34157-83-0 (castrol)  

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    Molecular Weight (MW)450.61
    FormulaC29H38O4
    CAS No.34157-83-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 90 mg/mL (199.7 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    InChi Key: KQJSQWZMSAGSHN-JJWQIEBTSA-N

    InChi Code: 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

    SMILES Code: O=C([[email protected]@](CC[[email protected]]1(C)CC[[email protected]]2(C)C3=CC=C4C(C)=C5O)(C)C[[email protected]@]1([H])[[email protected]]2(C)CC[[email protected]@]3(C)C4=CC5=O)O

    SynonymsCelastrol; Tripterin; Tripterine; 


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    In Vitro

    In vitro activity: Celastrol at 5 μM inhibits the chymotrypsin-like, PGPH-like, and trypsin-like activities of the purified 20S proteasome by 80%, 5%, and<1%, respectively, whereas at 10 μM, it inhibits these three proteasomal activities by ∼90%, 15%, and <1%, respectively. Celastrol significantly inhibits the proteasomal chymotrypsin activity in PC-3 cells in a concentration-dependent manner. Celastrol at 2.5 μM to 5 μM induces caspase-3 activity by 4.7-fold to 5.5-fold in PC-3 cells. Celastrol (5 μM) treated cells, the levels of the proteasome target proteins, IκB-α and Bax, are increased after 1 hour and further increased to its peak for 4 hours to 12 hours. Celastrol (2.5 μM) treatment induces proteasome inhibition by 40%, as shown by the decreased levels of chymotrypsin-like activity and increased accumulation of ubiquitinated proteins in LNCaP cells. Celastrol (2.5 μM) induces apoptosis in the Celastrol-treated LNCaP cells, as shown by increased levels of caspase-3 activity (up to 3.5-fold), PARP cleavage, and apoptotic morphology. Celastrol (300 nM) is found to suppress LPS-induced production of TNF-alpha and IL-1beta by human monocytes and macrophages. Celastrol (100 nM) also decreases LPS-induced expression of class II MHC molecules by microglia. Celastrol strongly inhibits LPS and IFN-y-induced NO production with IC50 of 200 nM in macrophage lineage cells. Celastrol strongly inhibits TNF-α and IFN-γ-induced NO production with IC50 of 200 nM in endothelial cells.


    Kinase Assay: 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 Assay: 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.

    In VivoCelastrol (3 mg/kg) results in significant inhibition (up to 70%) of tumor growth in male nude mice bearing PC-3 tumors, associated with increased p27 levels and Bax level. Celastrol (3 mg/kg) results more apoptotic tumor cells with the appearance of various PARP cleavage fragments in tumor of male nude mice bearing PC-3 tumors. Celastrol (3 mg/kg) causes 35% of tumor inhibition, associated with decreased proteasome activity and decreased expression of AR protein in nude mice bearing C4-2B tumors. Celastrol (3 mg/kg) is found to suppress strongly joint swelling and other manifestations of adjuvant arthritis in mice. Celastrol (0.2 mg/kg) significantly improves the performance in memory, learning and psychomotor activity tests in rats.
    Animal modelNude mice bearing C4-2B tumors
    Formulation & DosageDissolved in 10% DMSO, 70% Cremophor/ethanol (3:1), and 20% PBS; 3 mg/kg; i.p. administration
    References

    Cancer Res. 2006 May 1;66(9):4758-65; Prog Neuropsychopharmacol Biol Psychiatry. 2001 Oct;25(7):1341-57.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     

    CELASTROL

    Inhibition of the chymotrypsin-like activity of a purified rabbit 20S proteasome activity by Celastrol. Cancer Res. 2006 May 1;66(9):4758-65.
     

    CELASTROL

    Dosage-effects of Celastrol on PC-3 cells.  Cancer Res. 2006 May 1;66(9):4758-65.
     

    CELASTROL

    Kinetic studies on proteasome inhibition and apoptosis induction by Celastrol in PC-3 cells. Cancer Res. 2006 May 1;66(9):4758-65.
     

    CELASTROL

    Dosage and kinetic effects of Celastrol on LNCaP cells. Cancer Res. 2006 May 1;66(9):4758-65.
     

    CELASTROL

    Proteasome-inhibitory and antitumor effects of Celastrol in vivo. Cancer Res. 2006 May 1;66(9):4758-65.
     

    CELASTROL

    Immunohistochemistry and TUNEL assay using mouse tumor samples. Cancer Res. 2006 May 1;66(9):4758-65.


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