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 NUDvVXd1SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MmfTRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCSQ{OgZ4VtdCCuaX7lMEBKSzVyIE2gNE4xODFizszNMi=> M{fTVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4Nki2OVM4Lz5zNk[4OlU{PzxxYU6=
WM266.4 NF7seVREgXSxdH;4bYNqfHliYYPzZZk> NX;sd2hFPzJiaILz M{LZR2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHdOOjZ4LkSgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEGWUHzpeIUh[XO|YYmsJGlEPTBiPTCwMlAxPDhizszNMi=> MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJyNki2PUc,OjJ{ME[4Olk9N2F-
lymphoblastoid cells NWjhcJRmTnWwY4Tpc44h[XO|YYm= M2X6R2lvcGmkaYTpc44hd2ZiY3j5cY91enmyc3nuJIxqc2ViMkDTJJBzd3SnYYPvcYUh[WO2aY\peJkhcW5ibIntdIhw[myjc4TvbYQh[2WubIOsJGlEPTBiPTCwMlAxPSEQvF2u MkKyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd7OU[5PFcoRjF5OUm2PVg4RC:jPh?=
LCL NGHOO4NHfW6ldHnvckBie3OjeR?= M{O4[FEzKGi{cx?= M2Ti[2lvcGmkaYTpc44hd2ZiY3j5cY91enmyc3nuMYxqc2ViYXP0bZZqfHlib3[gNlBUKHC{b4TlZZNwdWViYnX0ZVIhcW5iaIXtZY4hVEOOIHPlcIx{KGGodHXyJFEzKGi{czygTWM2OCB;IECuNFA2KM7:TT6= NED2eYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{ME[4O|YxQSd-MkC2PFc3ODl:L3G+
DLD1 MVrGeY5kfGmxbjDhd5NigQ>? MXm2JIhzew>? M1vlNmlvcGmkaYTpc44hd2ZiY3j5cY91enmyc3nuMYxqc2ViYXP0bZZqfHlib3[gNlBUKHC{b4TlZZNwdWViaX6gbJVu[W5iRFzENUBk\WyuczD0doFve2[nY4Tl[EB4cXSqIETVZk1NfWNiZ3Xu[UB2e2mwZzDTeYNkcW67bD3M[ZUuVGW3LW\hcE1VgXJvQV3DJIF{KHO3YoP0doF1\SCjZoTldkA3KGi{czDifUB{eGWldILv[ox2d3KxbXX0dolkKGGwYXz5d4l{NCCLQ{WwJF0hOC5yME[g{txONg>? NXnlNIhpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNFY5PjlpPkKyNlA3QDZ7PD;hQi=>
HEK293 MmWySpVv[3Srb36gZZN{[Xl? NFvuUmszKGi{cx?= M2P1[WlvcGmkaYTpc44hd2ZiY3j5cY91enmyc3nuMYxqc2ViYXP0bZZqfHlib3[gdJJwfGWjc3;t[UBj\XSjLUWgd5VjfW6rdDDpckBJTUt{OUOgZ4VtdHNidYPpcochW3WlLVzMWnkuT2yxIHHzJJN2[nO2cnH0[UBqdmO3YnH0[YQh\m:{IEKgbJJ{KHC{aX;yJJRwKHO3YoP0doF1\SCjZHTpeIlwdiCvZXHzeZJm\CCjZoTldkAyOCCvaX7zJIJ6KGOnbHytZoF{\WRicILveIVie2:vZT3HcI8h[mW2YUWgZZN{[XluIFnDOVAhRSByLkCyOkDPxE1w NF3uUVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{W0NFc6OCd-MkO1OFA4QTB:L3G+
DLD1 MYPGeY5kfGmxbjDhd5NigQ>? NWj3OohUPiCqcoO= MYHJcohq[mm2aX;uJI9nKHCncITp[IUu\2y3dHHtfYwueGWydHnk[U1pgWS{b3z5folv\yCjY4Tpeol1gSCxZjCyNHMheHKxdHXhd49u\SCrbjDoeY1idiCGTFSxJINmdGy|IITyZY5{\mWldHXkJJdqfGhiNGXiMWx2[yCpZX7lJJV{cW6pIGqtUIV2NUyndT3HcJUuSU2FIHHzJJN2[nO2cnH0[UBi\nSncjC2JIhzeyCkeTDzdIVkfHKxZnz1c5JwdWW2cnnjJIFv[Wy7c3nzMEBKSzVyIE2gNE4xPiEQvF2u M1;sXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkC2PFY6Lz5{MkKwOlg3QTxxYU6=
lymphoblastoid cells NH;4VnNHfW6ldHnvckBie3OjeR?= M2fTZ2lvcGmkaYTpc44hd2ZidIL5dJNqdiCuaXvlJFIxWyCycn;0[YF{d22nIHHjeIl3cXS7IHnuJIx6dXCqb3LsZZN1d2mmIHPlcIx{NCCLQ{WwJF0hOC5{OESg{txONg>? MnXnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd7OU[5PFcoRjF5OUm2PVg4RC:jPh?=
LCL M4\Zd2Z2dmO2aX;uJIF{e2G7 Mn;0NVIhcHK| NHjTTWlKdmirYnn0bY9vKG:oIITyfZB{cW5vbHnr[UBi[3Srdnn0fUBw\iB{MGOgdJJwfGWjc3;t[UBj\XSjMjDpckBpfW2jbjDMR2wh[2WubIOgZYZ1\XJiMUKgbJJ{NCCLQ{WwJF0hOC5{OESg{txONg>? MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODZ6N{[wPUc,OjB4OEe2NFk9N2F-
HEK293 MXLGeY5kfGmxbjDhd5NigQ>? M{nPUlIhcHK| MYHJcohq[mm2aX;uJI9nKHCxc4ThZ4llKGGldHn2bZR6KG:oIEKwd{Bxem:2ZXHzc41mKGKndHGtNUB{fWK3bnn0JIlvKEiHS{K5N{Bk\WyuczD1d4lv\yCcLX7MVI5NTC2JbH:gZZMhe3Wkc4TyZZRmKGmwY4XiZZRm\CCob4KgNkBpenNicILpc5IhfG9ic4Xid5Rz[XSnIHHk[Il1cW:wIH3lZZN2emWmIHHmeIVzKDFyIH3pcpMh[nliY3XscE1j[XOnZDDwdo91\WG|b33lMWdtdyCkZYThNUBie3OjeTygTWM2OCB;IECuN{DPxE1w MljuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3NEC3PVAoRjJ|NUSwO|kxRC:jPh?=
KB-8-5-11 NYXF[FZbTnWwY4Tpc44h[XO|YYm= MYnQMYdtgWOxcILveIVqdiC|dXLzeJJifGW|IHnk[Y51cW[rZXSgbY4hU0JvOD21MVEyKGGmZX7vZ4Fz[2mwb33hJINmdGxibHnu[UwheUiWUzD0bIVz[XCndYTpZ{BtcWK{YYL5JJNkemWnbjygVI91\W6leTC9JFIvPTl{OTFOwG0v MkfWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF3MUWyPFQoRjNzNUG1Nlg1RC:jPh?=
lymphoblastoid cells M2D0fWZ2dmO2aX;uJIF{e2G7 NETFZXRKdmirYnn0bY9vKG:oIHPhd5Bie2VibHnr[UAzOFNicILveIVie2:vZTDhZ5Rqfmm2eTDpckBtgW2yaH;icIF{fG:rZDDj[YxteyxiSVO1NEA:KDRwNU[g{txONg>? MnvZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd7OU[5PFcoRjF5OUm2PVg4RC:jPh?=
LCL M{\UWGZ2dmO2aX;uJIF{e2G7 M3rIfFEzKGi{cx?= NVjz[ppsUW6qaXLpeIlwdiCxZjDQS3BJKGOjdHHsfZRq[yCjY4Tpeol1gSCxZjCyNHMheHKxdHXhd49u\SCkZYThNkBqdiCqdX3hckBNS0xiY3XscJMh[W[2ZYKgNVIhcHK|LDDJR|UxKD1iND61OkDPxE1w MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODZ6N{[wPUc,OjB4OEe2NFk9N2F-
KB-3-1 NUXLOJNiTnWwY4Tpc44h[XO|YYm= MUjQMYdtgWOxcILveIVqdiC|dXLzeJJifGW|IHnk[Y51cW[rZXSgbY4hU0JvMz2xJIFl\W6xY3HyZ4lvd22jIHPlcIwhdGmwZTygdWhVWyC2aHXyZZBmfXSrYzDsbYJz[XK7IIPjdoVmdg>? NGHONWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUWxOVI5PCd-M{G1NVUzQDR:L3G+
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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