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Product name : Epoxomicin (Synonyms: BU-4061T)
Item : c3256
Price : 200mg, $1750;500mg, $2890; 1g, $3950;
contact : Send inquiry to: info@acesobio.com
CAS : 134381-21-8
Molecular Weight : 554.72
Formula : C28H50N4O7
Storage : at -20°C
Additional information : We offer significant discount for bulky quantity order.
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Details:
Description of:Epoxomicin (Synonyms: BU-4061T)
Epoxomicin(CAS:134381-21-8)is an irreversible, selective proteasome inhibitor.
IC50 value: Target: 20S proteasome in vitro: Epoxomicin inhibits proteasome activity in cell growth assays with an IC50 value of 4 nM and demonstrates potent cytotoxicity against B16-F10, HCT116, and Moser solid tumor cells, as well as P388 and K562 leukemia cells with IC50 values ranging from 2-44 nM [1] [2].

Quality control data:
Quality control by 1H-NMR, 13C-NMR, HPLC and LCMS.
Product will be shipped with supporting analytical data. 

REFERENCES

1: Kerns K, Morales P, Sutovsky P. Regulation of Sperm Capacitation by the 26S Proteasome: An Emerging New Paradigm in Spermatology. Biol Reprod. 2016 May;94(5):117. doi: 10.1095/biolreprod.115.136622. Epub 2016 Apr 6. Review. PubMed PMID: 27053366.

2: Newman DJ. Developing natural product drugs: Supply problems and how they have been overcome. Pharmacol Ther. 2016 Jun;162:1-9. doi: 10.1016/j.pharmthera.2015.12.002. Epub 2015 Dec 17. Review. PubMed PMID: 26706239.

3: Carmony KC, Kim KB. Activity-based imaging probes of the proteasome. Cell Biochem Biophys. 2013 Sep;67(1):91-101. doi: 10.1007/s12013-013-9626-4. Review. PubMed PMID: 23700161; PubMed Central PMCID: PMC3758798.

4: Kim KB, Crews CM. From epoxomicin to carfilzomib: chemistry, biology, and medical outcomes. Nat Prod Rep. 2013 May;30(5):600-4. doi: 10.1039/c3np20126k. Review. PubMed PMID: 23575525; PubMed Central PMCID: PMC3815659.

5: Morales P, Díaz ES, Kong M. Proteasome activity and its relationship with protein phosphorylation during capacitation and acrosome reaction in human spermatozoa. Soc Reprod Fertil Suppl. 2007;65:269-73. Review. PubMed PMID: 17644968.

6: Ceravolo R, Sgadò P, Frosini D, Corsini GU. Assessing neuroprotection in Parkinson's disease: from the animal models to molecular neuroimaging in vivo. J Neural Transm Suppl. 2006;(71):133-41. Review. PubMed PMID: 17447424.

7: Granot Z, Melamed-Book N, Bahat A, Orly J. Turnover of StAR protein: roles for the proteasome and mitochondrial proteases. Mol Cell Endocrinol. 2007 Feb;265-266:51-8. Epub 2007 Jan 10. Review. PubMed PMID: 17218054.

8: Gough JD, Crews CM. Probing protein function with small molecules. Ernst Schering Res Found Workshop. 2006;(58):61-74. Review. PubMed PMID: 16708999.

9: Kawate H, Ohnaka K, Takayanagi R. [Development of BMP-related drugs]. Nihon Rinsho. 2005 Oct;63 Suppl 10:463-6. Review. Japanese. PubMed PMID: 16279683.

10: Groll M, Huber R. Inhibitors of the eukaryotic 20S proteasome core particle: a structural approach. Biochim Biophys Acta. 2004 Nov 29;1695(1-3):33-44. Review. PubMed PMID: 15571807.


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