GSK-461364 - CAS 929095-18-1
Catalog number: B0084-307746
Category: Inhibitor
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Polo-like Kinase (PLK)
GSK-461364 is a Polo-like kinase 1 inhibitor, is also a small molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor GSK461364 selectively inhibits Plk1, inducing selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. Plk1, named after the polo gene of Drosophila melanogaster, is a serine/threonine protein kinase involved in regulating mitotic spindle function in a non-ATP competitive manner.
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Catalog Number Size Price Stock Quantity
B0084-307746 10 mg $149 In stock
B0084-307746 50 mg $498 In stock
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GSK461364; GSK 461364; GSK-461364; GSK461364A; GSK 461364A; GSK-461364A. 5-[6-[(4-Methyl-1-piperazinyl)methyl]-1h-benzimidazol-1-yl]-3-[(1r)-1-[2-(trifluoromethyl)phenyl]ethoxy]-2-thiophenecarboxamide
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1.BI 6727 and GSK461364 suppress growth and radiosensitize osteosarcoma cells, but show limited cytotoxic effects when combined with conventional treatments.
Bogado RF;Pezuk JA;de Oliveira HF;Tone LG;Brassesco MS Anticancer Drugs. 2015 Jan;26(1):56-63. doi: 10.1097/CAD.0000000000000157.
Polo-like kinase 1 (PLK1), a key regulator of mitosis, is often overexpressed in childhood cancers and is associated with poor prognosis. Previous reports have shown that inhibition of PLK1 might serve as a promising anticancer treatment for osteosarcoma. In this study, we tested the second-generation PLK1 inhibitors BI 6727 and GSK461364 in HOS and MG-63 cell lines, both as a single agent and in combination with methotrexate, cisplatin, vinblastine, doxorubicin, or ionizing radiation. Both PLK1 inhibitors worked equally in terms of cell growth arrest, apoptosis induction, and radiosensitization. Combining BI 6727 or GSK461364 with conventional treatments, however, showed trivial synergistic antitumor effects in vitro. Our results reinforce the potential use of PLK1 inhibitors for a pharmacologic intervention in osteosarcoma, although their applicability in polychemotherapeutic regimens deserves further investigation.
2.A high-content small molecule screen identifies sensitivity of glioblastoma stem cells to inhibition of polo-like kinase 1.
Danovi D;Folarin A;Gogolok S;Ender C;Elbatsh AM;Engström PG;Stricker SH;Gagrica S;Georgian A;Yu D;U KP;Harvey KJ;Ferretti P;Paddison PJ;Preston JE;Abbott NJ;Bertone P;Smith A;Pollard SM PLoS One. 2013 Oct 30;8(10):e77053. doi: 10.1371/journal.pone.0077053. eCollection 2013.
Glioblastoma multiforme (GBM) is the most common primary brain cancer in adults and there are few effective treatments. GBMs contain cells with molecular and cellular characteristics of neural stem cells that drive tumour growth. Here we compare responses of human glioblastoma-derived neural stem (GNS) cells and genetically normal neural stem (NS) cells to a panel of 160 small molecule kinase inhibitors. We used live-cell imaging and high content image analysis tools and identified JNJ-10198409 (J101) as an agent that induces mitotic arrest at prometaphase in GNS cells but not NS cells. Antibody microarrays and kinase profiling suggested that J101 responses are triggered by suppression of the active phosphorylated form of polo-like kinase 1 (Plk1) (phospho T210), with resultant spindle defects and arrest at prometaphase. We found that potent and specific Plk1 inhibitors already in clinical development (BI 2536, BI 6727 and GSK 461364) phenocopied J101 and were selective against GNS cells. Using a porcine brain endothelial cell blood-brain barrier model we also observed that these compounds exhibited greater blood-brain barrier permeability in vitro than J101. Our analysis of mouse mutant NS cells (INK4a/ARF(-/-), or p53(-/-)), as well as the acute genetic deletion of p53 from a conditional p53 floxed NS cell line, suggests that the sensitivity of GNS cells to BI 2536 or J101 may be explained by the lack of a p53-mediated compensatory pathway.
3.Plk1 inhibition leads to a failure of mitotic division during the first mitotic division in pig embryos.
Zhang Z;Chen C;Cui P;Liao Y;Yao L;Zhang Y;Rui R;Ju S J Assist Reprod Genet. 2017 Mar;34(3):399-407. doi: 10.1007/s10815-016-0864-4. Epub 2017 Jan 10.
PURPOSE: ;This study was conducted to examine the dynamic distribution of polo-like 1 kinase (Plk1) and the possible role it plays in first mitotic division during early porcine embryo development.;METHODS: ;Indirect immunofluorescence and confocal microscopy imaging techniques combined with western blot analyses were used to study the dynamic expression and subcellular localization of Plk1 protein in pig parthenogenetic embryos. Finally, a selective Plk1 inhibitor, GSK461364, was used to evaluate the potential role of Plk1 during this special stage.;RESULTS: ;The results showed that Plk1 upon expression exhibited specific dynamic intracellular localization, which closely correlated with the α-tubulin distribution during the first mitotic division. GSK461364 treatment resulted in cleavage failure, with majority of the GSK461364-treated embryos being arrested in prometaphase. Further results of the subcellular structure examination showed that GSK461364 treatment led to a significantly higher proportion of the treated embryos having abnormal spindles and misarranged chromosomes at the prometaphase stage.;CONCLUSIONS: ;Thus, these results indicated that Plk1 is essential for porcine embryos to complete the first mitotic division.
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CAS 929095-18-1 GSK-461364

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