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 19 publications

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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 Mn7nRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NXzvXWdFSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubDDsbY5mNCCLQ{WwJF0hOC5yMEGg{txONg>? MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjZ6NkWzO{c,OTZ4OE[1N|c9N2F-
WM266.4 NWW1S|R6S3m2b4TvfIlkcXS7IHHzd4F6 NH;FZo44OiCqcoO= NXLWS3d5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hX01{Nk[uOEBk\WyuczDh[pRmeiB5MjDodpMh[nliQWTQcIl1\SCjc4PhfUwhUUN3MDC9JFAvODB2ODFOwG0v MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJyNki2PUc,OjJ{ME[4Olk9N2F-
lymphoblastoid cells MYPGeY5kfGmxbjDhd5NigQ>? MmnaTY5pcWKrdHnvckBw\iClaIntc5RzgXC|aX6gcIls\SB{MGOgdJJwfGWjc3;t[UBi[3Srdnn0fUBqdiCueX3wbI9jdGG|dH;p[EBk\WyuczygTWM2OCB;IECuNFA2KM7:TT6= M4e1bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5OUm2PVg4Lz5zN{m5Olk5PzxxYU6=
LCL NYHZTG0xTnWwY4Tpc44h[XO|YYm= Mk\0NVIhcHK| M{TzO2lvcGmkaYTpc44hd2ZiY3j5cY91enmyc3nuMYxqc2ViYXP0bZZqfHlib3[gNlBUKHC{b4TlZZNwdWViYnX0ZVIhcW5iaIXtZY4hVEOOIHPlcIx{KGGodHXyJFEzKGi{czygTWM2OCB;IECuNFA2KM7:TT6= NEDrS209[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{ME[4O|YxQSd-MkC2PFc3ODl:L3G+
DLD1 NFvzdHRHfW6ldHnvckBie3OjeR?= M4fPWFYhcHK| Mk\ZTY5pcWKrdHnvckBw\iClaIntc5RzgXC|aX6tcIls\SCjY4Tpeol1gSCxZjCyNHMheHKxdHXhd49u\SCrbjDoeY1idiCGTFSxJINmdGy|IITyZY5{\mWldHXkJJdqfGhiNGXiMWx2[yCpZX7lJJV{cW6pIGP1Z4NqdnmuLVzleU1N\XVvVnHsMXR6ei2DTVOgZZMhe3Wkc4TyZZRmKGGodHXyJFYhcHK|IHL5JJNx\WO2cn;mcJVwem:vZYTybYMh[W6jbInzbZMtKEmFNUCgQUAxNjByNjFOwG0v MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJyNki2PUc,OjJ{ME[4Olk9N2F-
HEK293 NF3TPXpHfW6ldHnvckBie3OjeR?= NIHBVYwzKGi{cx?= NGfoOpNKdmirYnn0bY9vKG:oIHPofY1wfHK7cIPpck1tcWunIHHjeIl3cXS7IH;mJJBzd3SnYYPvcYUh[mW2YT21JJN2[nWwaYSgbY4hUEWNMkmzJINmdGy|IIXzbY5oKFO3Yz3MUHZ[NUeubzDhd{B{fWK|dILheIUhcW6ldXLheIVlKG[xcjCyJIhzeyCycnnvdkB1dyC|dXLzeJJifGViYXTkbZRqd25ibXXhd5Vz\WRiYX\0[ZIhOTBibXnud{BjgSClZXzsMYJie2WmIIDyc5Rm[XOxbXWtS4xwKGKndHG1JIF{e2G7LDDJR|UxKD1iMD6wNlYh|ryPLh?= NYfyW|Y6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1OFA4QTBpPkKzOVQxPzlyPD;hQi=>
DLD1 M2ewUWZ2dmO2aX;uJIF{e2G7 M{XvXVYhcHK| NFTyPXlKdmirYnn0bY9vKG:oIIDldJRq\GVvZ3z1eIFugWxvcHXweIll\S2qeXTyc4x6gmmwZzDhZ5Rqfmm2eTDv[kAzOFNicILveIVie2:vZTDpckBpfW2jbjDEUGQyKGOnbHzzJJRz[W6|ZnXjeIVlKHerdHigOHVjNUy3YzDn[Y5mKHW|aX7nJHouVGW3LVzleU1IdHVvQV3DJIF{KHO3YoP0doF1\SCjZoTldkA3KGi{czDifUB{eGWldILv[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwJF0hOC5yNjFOwG0v NILzWGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKwOlg3QSd-MkKyNFY5Pjl:L3G+
lymphoblastoid cells NFnDXXRHfW6ldHnvckBie3OjeR?= NIfQWGtKdmirYnn0bY9vKG:oIITyfZB{cW5ibHnr[UAzOFNicILveIVie2:vZTDhZ5Rqfmm2eTDpckBtgW2yaH;icIF{fG:rZDDj[YxteyxiSVO1NEA:KDBwMki0JO69VS5? M1HpSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5OUm2PVg4Lz5zN{m5Olk5PzxxYU6=
LCL MX7GeY5kfGmxbjDhd5NigQ>? NUGxO3hqOTJiaILz MnrMTY5pcWKrdHnvckBw\iC2conwd4lvNWyra3WgZYN1cX[rdImgc4YhOjCVIIDyc5Rm[XOxbXWgZoV1[TJiaX6gbJVu[W5iTFPMJINmdGy|IHHmeIVzKDF{IHjyd{whUUN3MDC9JFAvOjh2IN88UU4> M2XuTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNki3OlA6Lz5{ME[4O|YxQTxxYU6=
HEK293 NFPSfYdHfW6ldHnvckBie3OjeR?= MVeyJIhzew>? MVTJcohq[mm2aX;uJI9nKHCxc4ThZ4llKGGldHn2bZR6KG:oIEKwd{Bxem:2ZXHzc41mKGKndHGtNUB{fWK3bnn0JIlvKEiHS{K5N{Bk\WyuczD1d4lv\yCcLX7MVI5NTC2JbH:gZZMhe3Wkc4TyZZRmKGmwY4XiZZRm\CCob4KgNkBpenNicILpc5IhfG9ic4Xid5Rz[XSnIHHk[Il1cW:wIH3lZZN2emWmIHHmeIVzKDFyIH3pcpMh[nliY3XscE1j[XOnZDDwdo91\WG|b33lMWdtdyCkZYThNUBie3OjeTygTWM2OCB;IECuN{DPxE1w MnvFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NEC3PVAoRjJ|NUSwO|kxRC:jPh?=
KB-8-5-11 M{DtdmZ2dmO2aX;uJIF{e2G7 NEPlXVdRNWeueXPvdJJwfGWrbjDzeYJ{fHKjdHXzJIll\W62aX\p[YQhcW5iS1KtPE02NTFzIHHk[Y5w[2G{Y3nuc41iKGOnbHygcIlv\SxicVjUV{B1cGW{YYDleZRq[yCuaXLyZZJ6KHOlcnXlckwhWG:2ZX7jfUA:KDJwNUmyPUDPxE1w M{nESFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUG1Nlg1Lz5|MUWxOVI5PDxxYU6=
lymphoblastoid cells MY\GeY5kfGmxbjDhd5NigQ>? MnnpTY5pcWKrdHnvckBw\iClYYPwZZNmKGyra3WgNlBUKHC{b4TlZZNwdWViYXP0bZZqfHliaX6gcJlueGixYnzhd5RwcWRiY3XscJMtKEmFNUCgQUA1NjV4IN88UU4> MoHmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd7OU[5PFcoRjF5OUm2PVg4RC:jPh?=
LCL M3nhW2Z2dmO2aX;uJIF{e2G7 NGrCV5gyOiCqcoO= NVHpbnlWUW6qaXLpeIlwdiCxZjDQS3BJKGOjdHHsfZRq[yCjY4Tpeol1gSCxZjCyNHMheHKxdHXhd49u\SCkZYThNkBqdiCqdX3hckBNS0xiY3XscJMh[W[2ZYKgNVIhcHK|LDDJR|UxKD1iND61OkDPxE1w MkXmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4OEe2NFkoRjJyNki3OlA6RC:jPh?=
KB-3-1 NXXNVYtbTnWwY4Tpc44h[XO|YYm= MljNVE1odHmlb4Dyc5RmcW5ic4Xid5Rz[XSnczDp[IVvfGmoaXXkJIlvKEuELUOtNUBi\GWwb3PhdoNqdm:vYTDj[YxtKGyrbnWsJJFJXFNidHjldoFx\XW2aXOgcIljemG{eTDzZ5Jm\W5? M1TVfVxiKHSjcnfleF0oZ2KuYX7rK{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

Solubility (25°C)

In vitro

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

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