247068-92-4
Chemical Structure
Biotin-(Oaa)3-epoxomicin
- CAS. Nr.: 247068-92-4
- Formula:C54H95N9O11S
- Molecular Weight:1078.45
IUPAC Name: N-((2S,3S)-1-(((2S,3S)-1-(((2S,3R)-3-hydroxy-1-(((S)-4-methyl-1-((R)-2-methyloxiran-2-yl)-1-oxopentan-2-yl)amino)-1-oxobutan-2-yl)amino)-3-methyl-1-oxopentan-2-yl)amino)-3-methyl-1-oxopentan-2-yl)-N-methyl-6-(6-(6-(5-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanamido)hexanamido)hexanamido)hexanamide
InChIKey: TWHRMHRNYSDMAU-LLLMMZAZSA-N
SMILES: O=C([C@]1(CO1)C)[C@H](CC(C)C)NC([C@H]([C@H](O)C)NC([C@H]([C@@H](C)CC)NC([C@H]([C@@H](C)CC)N(C)C(CCCCCNC(CCCCCNC(CCCCCNC(CCCC[C@H]2[C@]3([H])[C@](NC(N3)=O)([H])CS2)=O)=O)=O)=O)=O)=O)=O
Biological Activity: 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].
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Biotin-(Oaa)3-epoxomicin | 96.46% | 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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- [1]. Meng L, et al. Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity. Proc Natl Acad Sci U S A. 1999;96(18):10403-10408. [Content Brief]
- [2]. Hanada M, et al. Epoxomicin, a new antitumor agent of microbial origin. J Antibiot (Tokyo). 1992;45(11):1746-1752. [Content Brief]
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