Epoxomicin (BU-4061T)

Catalog No.S7038 Synonyms: Aids010837

For research use only.

Epoxomicin (BU-4061T, Aids010837) is a selective proteasome inhibitor with anti-inflammatory activity, inhibits primarily the CH-L activity of the 20S proteasome, while T-L and PGPH catalytic activities are also inhibited at 100- and 1000-fold reduced rate. Epoxomicin promotes apoptosis.

Epoxomicin (BU-4061T) Chemical Structure

CAS No. 134381-21-8

Selleck's Epoxomicin (BU-4061T) has been cited by 15 publications

Purity & Quality Control

Choose Selective Proteasome Inhibitors

Other Proteasome Products

Biological Activity

Description Epoxomicin (BU-4061T, Aids010837) is a selective proteasome inhibitor with anti-inflammatory activity, inhibits primarily the CH-L activity of the 20S proteasome, while T-L and PGPH catalytic activities are also inhibited at 100- and 1000-fold reduced rate. Epoxomicin promotes apoptosis.
Features Epoxomicin is a natural product isolated from an Actinomycetes species.
Targets
20S proteasome [1]
In vitro

Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome. Epoxomicin (100 nM) results in a 30-fold increase in the levels of p53 protein, a known target of the proteasome, in HUVECs. Epoxomicin (10 μM) results in the accumulation of ubiquitinated proteins in HeLa cells. Epoxomicin (10 μM) inhibits IκBα degradation by 10-fold in HeLa cells. Epoxomicin (10 μM) produces a significant dose-dependent reduction in TNF-α-stimulated NF-κB DNA-binding activity in HeLa cells. [1] Epoxomicin inhibits proliferating of EL4 lymphoma cells with biotinylated chimerae with IC50 of 4 nM. [2] Epoxomicin (1 μM) leads to a reduction of LCMV GP33 presentation and an enhancement of GP276 presentation. [3] Epoxomicin inhibits growth of Babesia bigemina with IC50 of 4 nM. Epoxomicin (0.5 mg/kg and 0.05 mg/kg) results in peak parasitemia levels of 34.8% and 42.3% in B. microti. [4] Epoxomicin (100 nM) decreases the total parasitemia by 78%, 86% and 77% in Plasmodium falciparum. Epoxomicin (10 μM) inhibits gametogenesis and exflagellation as well as development into oocysts of anopheles mosquitoes. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PC3 NGXLS2NCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MV;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxtKGyrbnWsJGlEPTBiPTCwMlAxOSEQvF2u MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjZ6NkWzO{c,OTZ4OE[1N|c9N2F-
WM266.4 NIfoTnNEgXSxdH;4bYNqfHliYYPzZZk> M{C5Z|czKGi{cx?= NFjvfXBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBYVTJ4Nj60JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCDVGDsbZRmKGG|c3H5MEBKSzVyIE2gNE4xODR6IN88UU4> MlW0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{ME[4OlkoRjJ{MkC2PFY6RC:jPh?=
lymphoblastoid cells M4rRPWZ2dmO2aX;uJIF{e2G7 MXrJcohq[mm2aX;uJI9nKGOqeX3veJJ6eHOrbjDsbYtmKDJyUzDwdo91\WG|b33lJIFkfGm4aYT5JIlvKGy7bYDoc4Jt[XO2b3nkJINmdGy|LDDJR|UxKD1iMD6wNFUh|ryPLh?= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzl7Nkm4O{c,OTd7OU[5PFc9N2F-
LCL MYXGeY5kfGmxbjDhd5NigQ>? NVXpUpdPOTJiaILz MoDGTY5pcWKrdHnvckBw\iClaIntc5RzgXC|aX6tcIls\SCjY4Tpeol1gSCxZjCyNHMheHKxdHXhd49u\SCkZYThNkBqdiCqdX3hckBNS0xiY3XscJMh[W[2ZYKgNVIhcHK|LDDJR|UxKD1iMD6wNFUh|ryPLh?= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODZ6N{[wPUc,OjB4OEe2NFk9N2F-
DLD1 MX3GeY5kfGmxbjDhd5NigQ>? M4PhNFYhcHK| M3\tVWlvcGmkaYTpc44hd2ZiY3j5cY91enmyc3nuMYxqc2ViYXP0bZZqfHlib3[gNlBUKHC{b4TlZZNwdWViaX6gbJVu[W5iRFzENUBk\WyuczD0doFve2[nY4Tl[EB4cXSqIETVZk1NfWNiZ3Xu[UB2e2mwZzDTeYNkcW67bD3M[ZUuVGW3LW\hcE1VgXJvQV3DJIF{KHO3YoP0doF1\SCjZoTldkA3KGi{czDifUB{eGWldILv[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwJF0hOC5yME[g{txONg>? Mn7RQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{ME[4OlkoRjJ{MkC2PFY6RC:jPh?=
HEK293 NIjTdlBHfW6ldHnvckBie3OjeR?= NUjQTplmOiCqcoO= NX;hfmxYUW6qaXLpeIlwdiCxZjDjbJlud3S{eYDzbY4udGmtZTDhZ5Rqfmm2eTDv[kBxem:2ZXHzc41mKGKndHGtOUB{fWK3bnn0JIlvKEiHS{K5N{Bk\WyuczD1d4lv\yCVdXOtUGxXYS2JbH:gZZMhe3Wkc4TyZZRmKGmwY4XiZZRm\CCob4KgNkBpenNicILpc5IhfG9ic4Xid5Rz[XSnIHHk[Il1cW:wIH3lZZN2emWmIHHmeIVzKDFyIH3pcpMh[nliY3XscE1j[XOnZDDwdo91\WG|b33lMWdtdyCkZYThOUBie3OjeTygTWM2OCB;IECuNFI3KM7:TT6= M2HIblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUSwO|kxLz5{M{W0NFc6ODxxYU6=
DLD1 NE\XbYRHfW6ldHnvckBie3OjeR?= MWS2JIhzew>? Mn7STY5pcWKrdHnvckBw\iCyZYD0bYRmNWeudYThcZltNXCncITp[IUucHmmcn;sfZpqdmdiYXP0bZZqfHlib3[gNlBUKHC{b4TlZZNwdWViaX6gbJVu[W5iRFzENUBk\WyuczD0doFve2[nY4Tl[EB4cXSqIETVZk1NfWNiZ3Xu[UB2e2mwZzDaMWxmfS2OZYWtS4x2NUGPQzDhd{B{fWK|dILheIUh[W[2ZYKgOkBpenNiYomgd5Bm[3S{b3\seY9zd22ndILpZ{BidmGueYPpd{whUUN3MDC9JFAvODZizszNMi=> NHn1RWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKwOlg3QSd-MkKyNFY5Pjl:L3G+
lymphoblastoid cells M1:2cWZ2dmO2aX;uJIF{e2G7 MoPQTY5pcWKrdHnvckBw\iC2conwd4lvKGyra3WgNlBUKHC{b4TlZZNwdWViYXP0bZZqfHliaX6gcJlueGixYnzhd5RwcWRiY3XscJMtKEmFNUCgQUAxNjJ6NDFOwG0v MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzl7Nkm4O{c,OTd7OU[5PFc9N2F-
LCL NELuSHVHfW6ldHnvckBie3OjeR?= NWDZcWRQOTJiaILz MWPJcohq[mm2aX;uJI9nKHS{eYDzbY4udGmtZTDhZ5Rqfmm2eTDv[kAzOFNicILveIVie2:vZTDi[ZRiOiCrbjDoeY1idiCOQ1ygZ4VtdHNiYX\0[ZIhOTJiaILzMEBKSzVyIE2gNE4zQDRizszNMi=> MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODZ6N{[wPUc,OjB4OEe2NFk9N2F-
HEK293 MlPlSpVv[3Srb36gZZN{[Xl? MYiyJIhzew>? MoDGTY5pcWKrdHnvckBw\iCyb4P0ZYNq\CCjY4Tpeol1gSCxZjCyNJMheHKxdHXhd49u\SCkZYThMVEhe3WkdX7peEBqdiCKRVuyPVMh[2WubIOgeZNqdmdiWj3uUHBvVERvR3zvJIF{KHO3YoP0doF1\SCrbnP1ZoF1\WRiZn;yJFIhcHK|IIDybY9zKHSxIIP1ZpN1emG2ZTDh[IRqfGmxbjDt[YF{fXKnZDDh[pRmeiBzMDDtbY5{KGK7IHPlcIwu[mG|ZXSgdJJwfGWjc3;t[U1IdG9iYnX0ZVEh[XO|YYmsJGlEPTBiPTCwMlMh|ryPLh?= M4TDW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUSwO|kxLz5{M{W0NFc6ODxxYU6=
KB-8-5-11 MojISpVv[3Srb36gZZN{[Xl? NWP6TI1FWC2pbInjc5Bzd3SnaX6gd5Vje3S{YYTld{Bq\GWwdHnmbYVlKGmwIFvCMVguPS1zMTDh[IVvd2OjcnPpco9u[SClZXzsJIxqdmVuIIHIWHMhfGincnHw[ZV1cWNibHnidoFzgSC|Y4Ll[Y4tKFCxdHXuZ5khRSB{LkW5Nlkh|ryPLh?= NFvORVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUWxOVI5PCd-M{G1NVUzQDR:L3G+
lymphoblastoid cells NHLHV5dHfW6ldHnvckBie3OjeR?= NX3CXWNjUW6qaXLpeIlwdiCxZjDjZZNx[XOnIHzpb4UhOjCVIIDyc5Rm[XOxbXWgZYN1cX[rdImgbY4hdHmvcHjvZoxie3SxaXSgZ4VtdHNuIFnDOVAhRSB2LkW2JO69VS5? M33nO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5OUm2PVg4Lz5zN{m5Olk5PzxxYU6=
LCL NGCy[YlHfW6ldHnvckBie3OjeR?= NXPkd3ViOTJiaILz NFG0R5pKdmirYnn0bY9vKG:oIGDHVGgh[2G2YXz5eIlkKGGldHn2bZR6KG:oIEKwV{Bxem:2ZXHzc41mKGKndHGyJIlvKGi3bXHuJGxEVCClZXzsd{Bi\nSncjCxNkBpenNuIFnDOVAhRSB2LkW2JO69VS5? MnHOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4OEe2NFkoRjJyNki3OlA6RC:jPh?=
KB-3-1 MYXGeY5kfGmxbjDhd5NigQ>? NEWwWVBRNWeueXPvdJJwfGWrbjDzeYJ{fHKjdHXzJIll\W62aX\p[YQhcW5iS1KtN{0yKGGmZX7vZ4Fz[2mwb33hJINmdGxibHnu[UwheUiWUzD0bIVz[XCndYTpZ{BtcWK{YYL5JJNkemWnbh?= M2HsZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUG1Nlg1Lz5|MUWxOVI5PDxxYU6=
In vivo Epoxomicin (0.58 mg/kg per day) reduces the CS response by 44% relative to the control group of mice treated with vehicle alone. Epoxomicin (2.9 mg/kg) potently inhibits the irritant-associated inflammatory response by 95% when ear edema measurements are made 24 hours postchallenge in mice. [1]

Protocol (from reference)

Animal Research:[1]
  • Animal Models: BALB/c mice
  • Dosages: 2.9 mg/kg
  • Administration: intraperitoneal injection
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(180.27 mM)
Water Insoluble
Ethanol '100 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 554.72
Formula

C28H50N4O7

CAS No. 134381-21-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC(C)C(C(=O)NC(C(C)O)C(=O)NC(CC(C)C)C(=O)C1(CO1)C)NC(=O)C(C(C)CC)N(C)C(=O)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Epoxomicin (BU-4061T) | Epoxomicin (BU-4061T) supplier | purchase Epoxomicin (BU-4061T) | Epoxomicin (BU-4061T) cost | Epoxomicin (BU-4061T) manufacturer | order Epoxomicin (BU-4061T) | Epoxomicin (BU-4061T) distributor