1. Metabolic Enzyme/Protease
    Apoptosis
  2. Proteasome
    Apoptosis
  3. Epoxomicin

Epoxomicin (Synonyms: BU-4061T)

Cat. No.: HY-13821 Purity: 98.81%
Handling Instructions

Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity.

For research use only. We do not sell to patients.

Epoxomicin Chemical Structure

Epoxomicin Chemical Structure

CAS No. : 134381-21-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 586 In-stock
Estimated Time of Arrival: December 31
100 μg USD 96 In-stock
Estimated Time of Arrival: December 31
1 mg USD 156 In-stock
Estimated Time of Arrival: December 31
5 mg USD 480 In-stock
Estimated Time of Arrival: December 31
10 mg USD 840 In-stock
Estimated Time of Arrival: December 31
20 mg USD 1320 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE Epoxomicin

    Epoxomicin purchased from MCE. Usage Cited in: Mol Plant Pathol. 2018 Dec;19(12):2623-2634.

    Destabilization of BRC1 mediated by SWP1 is inhibited by proteasome inhibitors Epoxomicin and MG132.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity[1][2][3][4][5].

    IC50 & Target

    Proteasome[1]

    In Vitro

    Epoxomicin shows quite potent cytotoxicities against all of the cells tested. Epoxomicin inhibits the cells growth of B16-F10, HCT116, Moser, P388 and K562 cells of IC50 values of 0.002 μg/mL, 0.005 μg/mL, 0.044 μg/mL, 0.002 μg/mL and 0.037 μg/mL[1].
    Epoxomicin has antiproliferative activity with an IC50 of 4 nM in EL4 lymphoma cells[2].

    In Vivo

    Epoxomicin (0.063-1 mg/kg; intraperitoneal injection; once daily; for 9 days; male BDFX mice) treatment shows significant antitumor effect with the minimumeffective dose of 0.13mg/kg/day[1].
    Epoxomicin also effectively inhibits NF-κB activation in vitro and potently blocks in vivo inflammation in the murine ear edema assay[3].
    Epoxomicin is injected into adult rats over a period of 2 weeks. After a latency of 1 to 2 weeks, animals developed progressive Parkinsonism with bradykinesia, rigidity, tremor, and an abnormal posture. Postmortem analyses shows striatal dopamine depletion and dopaminergic cell death with apoptosis in the substantia nigra pars compacta[4].

    Animal Model: Male BDFX mice with B16 melanoma[1]
    Dosage: 0.063 mg/kg, 0.13 mg/kg, 0.25 mg/kg, 0.5 mg/kg, 1 mg/kg
    Administration: Intraperitoneal injection; once daily; for 9 days
    Result: Exhibited strong therapeutic activity against B16 melanoma.
    Molecular Weight

    554.72

    Formula

    C₂₈H₅₀N₄O₇

    CAS No.

    134381-21-8

    SMILES
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (180.27 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8027 mL 9.0136 mL 18.0271 mL
    5 mM 0.3605 mL 1.8027 mL 3.6054 mL
    10 mM 0.1803 mL 0.9014 mL 1.8027 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.51 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (4.51 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.51 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 98.81%

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    Keywords:

    EpoxomicinBU-4061TProteasomeApoptosisEpoxyketone-containingantitumorantiproliferativecytotoxicitiesanti-inflammatoryBBBParkinson'scovalentlyInhibitorinhibitorinhibit

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    Cat. No.:
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