1. Metabolic Enzyme/Protease NF-κB
  2. Proteasome NF-κB
  3. Biotin-(Oaa)3-epoxomicin

Biotin-(Oaa)3-epoxomicin is a biotin-labeled form of Epoxomicin (HY-13821), prepared by conjugating Epoxomicin with biotin via three hydrophilic oxaacetyl amino acid (Oaa) linkers. Biotin-(Oaa)3-epoxomicin is primarily used in proteomic studies for the capture, identification and target validation of proteasome complexes, to determine the intracellular targets of epoxomicin. Epoxomicin acts as a proteasome inhibitor and NF-κB inhibitor, which effectively blocks inflammatory responses in mouse ear edema assays. It inhibits proteasome activity via covalent binding to catalytic subunits including LMP7, X, MECL1 and Z, with the strongest inhibitory effect on chymotrypsin-like activity, and does not interfere with non-proteasomal proteases such as trypsin and papain.

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Biotin-(Oaa)3-epoxomicin

Biotin-(Oaa)3-epoxomicin Chemical Structure

CAS No. : 247068-92-4

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Description

Biotin-(Oaa)3-epoxomicin is a biotin-labeled form of Epoxomicin (HY-13821), prepared by conjugating Epoxomicin with biotin via three hydrophilic oxaacetyl amino acid (Oaa) linkers. Biotin-(Oaa)3-epoxomicin is primarily used in proteomic studies for the capture, identification and target validation of proteasome complexes, to determine the intracellular targets of epoxomicin. Epoxomicin acts as a proteasome inhibitor and NF-κB inhibitor, which effectively blocks inflammatory responses in mouse ear edema assays. It inhibits proteasome activity via covalent binding to catalytic subunits including LMP7, X, MECL1 and Z, with the strongest inhibitory effect on chymotrypsin-like activity, and does not interfere with non-proteasomal proteases such as trypsin and papain[1][2].

In Vitro

Epoxomicin (5-8 μM; 4 hr) covalently binds to the LMP7, MECL1, Z, and X catalytic β subunits of the proteasome in EL4 murine thymoma cells and LCL 721.45/LCL 721.174 human B cell lymphoma cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

1078.45

Formula

C54H95N9O11S

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Biotin-{Oaa}-{Oaa}-{Oaa}-Ile-Ile-Thr-{Leu((2R)-2-methyloxiranyl)}

Sequence Shortening

Biotin-{Oaa}-{Oaa}-{Oaa}-IIT-{Leu((2R)-2-methyloxiranyl)}

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (92.73 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9273 mL 4.6363 mL 9.2726 mL
5 mM 0.1855 mL 0.9273 mL 1.8545 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9273 mL 4.6363 mL 9.2726 mL 23.1814 mL
5 mM 0.1855 mL 0.9273 mL 1.8545 mL 4.6363 mL
10 mM 0.0927 mL 0.4636 mL 0.9273 mL 2.3181 mL
15 mM 0.0618 mL 0.3091 mL 0.6182 mL 1.5454 mL
20 mM 0.0464 mL 0.2318 mL 0.4636 mL 1.1591 mL
25 mM 0.0371 mL 0.1855 mL 0.3709 mL 0.9273 mL
30 mM 0.0309 mL 0.1545 mL 0.3091 mL 0.7727 mL
40 mM 0.0232 mL 0.1159 mL 0.2318 mL 0.5795 mL
50 mM 0.0185 mL 0.0927 mL 0.1855 mL 0.4636 mL
60 mM 0.0155 mL 0.0773 mL 0.1545 mL 0.3864 mL
80 mM 0.0116 mL 0.0580 mL 0.1159 mL 0.2898 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Biotin-(Oaa)3-epoxomicin
Cat. No.:
HY-P11306
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