Poloxin
Poloxin is the first small-molecule inhibitor specifically targeting the function of the Plk1 PBD. Poloxin induces centrosome fragmentation and abnormal spindle and chromosome misalignment, which activate the spindle assembly checkpoint and prolong mitosis. Notably, centrosomal fragmentation induced by Poloxin is partially attributable to dysfunctional Kizuna, a key substrate of Plk1 at centrosomes. Moreover, Poloxin strongly inhibits proliferation of a panel of cancer cells by inducing mitotic arrest, followed by a surge of apoptosis. More important, we report, for the first time to our knowledge, that the PBD inhibitor, Poloxin , significantly suppresses tumor growth of cancer cell lines in xenograft mouse models by lowering the proliferation rate and triggering apoptosis in treated tumor tissues. Targeting the PBD by Poloxin is a powerful approach for selectively inhibiting Plk1 function in vitro and in vivo. ( Am J Pathol. 2011 Oct;179(4):2091-9. ). (2/18/2014)
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Chemical Information
| Name | Poloxin |
|---|---|
| Iupac Chemical Name | (E)-4-isopropyl-3,6-dioxocyclohexa-1,4-dienecarbaldehyde O-(2-methylbenzoyl) oxime. |
| Synonyms | Poloxin |
| Molecular Formula | C18H17NO4 |
| Molecular Weight | 311.33 |
| Smile | O=C(C(/C=N/OC(C1=CC=CC=C1C)=O)=C2)C=C(C(C)C)C2=O |
| InChiKey | KRHMAJOTJVOLBI-VXLYETTFSA-N |
| InChi | InChI=1S/C18H17NO4/c1-11(2)15-9-16(20)13(8-17(15)21)10-19-23-18(22)14-7-5-4-6-12(14)3/h4-11H,1-3H3/b19-10+ |
| CAS Number | 321688-88-4 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
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| Bulk | Enquiry | Enquiry | Enquiry |
| Purity | 98% Min. |
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1: Sanhaji M, Louwen F, Zimmer B, Kreis NN, Roth S, Yuan J. Polo-like kinase 1 inhibitors, mitotic stress and the tumor suppressor p53. Cell Cycle. 2013 May 1;12(9):1340-51. doi: 10.4161/cc.24573. Epub 2013 Apr 10. PubMed PMID: 23574746; PubMed Central PMCID: PMC3674062.
2: Weiß L, Efferth T. Polo-like kinase 1 as target for cancer therapy. Exp Hematol Oncol. 2012 Dec 10;1(1):38. doi: 10.1186/2162-3619-1-38. PubMed PMID: 23227884; PubMed Central PMCID: PMC3533518.
3: Sanhaji M, Kreis NN, Zimmer B, Berg T, Louwen F, Yuan J. p53 is not directly relevant to the response of Polo-like kinase 1 inhibitors. Cell Cycle. 2012 Feb 1;11(3):543-53. doi: 10.4161/cc.11.3.19076. Epub 2012 Feb 1. PubMed PMID: 22262171.
4: Yuan J, Sanhaji M, Krämer A, Reindl W, Hofmann M, Kreis NN, Zimmer B, Berg T, Strebhardt K. Polo-box domain inhibitor poloxin activates the spindle assembly checkpoint and inhibits tumor growth in vivo. Am J Pathol. 2011 Oct;179(4):2091-9. doi: 10.1016/j.ajpath.2011.06.031. Epub 2011 Aug 10. PubMed PMID: 21839059; PubMed Central PMCID: PMC3181368.
5: Liao C, Park JE, Bang JK, Nicklaus MC, Lee KS. Exploring Potential Binding Modes of Small Drug-like Molecules to the Polo-Box Domain of Human Polo-like Kinase 1. ACS Med Chem Lett. 2010;1(3):110-114. PubMed PMID: 20625469; PubMed Central PMCID: PMC2898210.
6: Reindl W, Yuan J, Krämer A, Strebhardt K, Berg T. Inhibition of polo-like kinase 1 by blocking polo-box domain-dependent protein-protein interactions. Chem Biol. 2008 May;15(5):459-66. doi: 10.1016/j.chembiol.2008.03.013. PubMed PMID: 18482698.
7: Lee KS, Idle JR. Pinning down the polo-box domain. Chem Biol. 2008 May;15(5):415-6. doi: 10.1016/j.chembiol.2008.04.009. PubMed PMID: 18482691.
Chemical Structure
