Polo-like Kinase (PLK)|Inhibitors Agonists Modulators Antagonists|HmoBio.com

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Polo-like Kinases (PLKs) are important regulators of the cell cycle. Plks are involved in the formation of and the changes in the mitotic spindle and in the activation of CDK/cyclin complexes during M-phase of the cell cycle.Polo-like kinases (Plks) are a family of conserved serine/threonine kinases involved in the regulation of cell cycle progression through G2 and mitosis. Mammalian polo-like kinases include Plk1 (Xenopus Plx1), Plk2/Snk (Xenopus Plx2), Plk3/Prk/FnK (Xenopus Plx3), Plk4/Sak and Plk5. Plk1 is involved in the regulation of key steps during cell division, DNA damage repair pathways, apoptosis, and the progression of the cell cycle. Plk3 is a multifunctional stress response protein that responses to signals induced by DNA damage and/or mitotic spindle disruption.

Cat. No.	Product Name	CAS No.	Information
H2248	Volasertib	755038-65-4	Volasertib (BI 6727) is a potent, selective Polo-like kinase (PLK) inhibitor with IC50 of 0.87, 5 and 56 nM for PLK1, 2 and 3, respectively; displays no inhibitory activity against a panel of >50 other kinases; inhibits proliferation of multiple cell lines derived from various cancer tissues, including HCT116 (EC50=23 nM) and NCI-H460 (EC50=21 nM),BRO (EC50=11 nM), and hematopoietic cancer cell HL-60 (EC50=32 nM); demonstrates marked antitumor activity in multiple cancer models, including a model of taxane-resistant colorectal cancer.
H2247	T-521	891020-54-5	T-521 is a novel PLK1 PBD (Polo-box domain) inhibitor that specifically inhibits the PBD of PLK1 (IC50=1.22 uM), but not those of Plk2-3; impedes the interaction between Plk1 and Bub1, exhibits dramatic mitotic defects in HeLa cells; suppresses the growth of A549 cells in xenograft nude mice.
H2246	Scytonemin	152075-98-4	Scytonemin is a marine natural product that inhibits PLK1 with IC50 of 2 uM against recombinant enzyme, shows similar potentcy for Myt1, Chk1,Cdk1/cyclin B and PKCβ2, less potent against PKA and Tie2; effectively attenuates the growth factor- or mitogen-induced proliferation of cells in inflammatory hyperproliferation, without chemical toxicity; induces apoptosis in Jurkat T cells.
H2245	Rigosertib sodium	592542-60-4	Rigosertib sodium (ON 01910.Na) is a potent, non-ATP-competitive PLK1 inhibitor (IC50=9-10 nM), selectively induces mitotic G2/M arrest and apoptosis in cancer cells; also exhibits inhibitory activity against PDGFR, Abl, and Flt-1, at higher concentrations, inhibits CDK1, Plk2, Src, and Fyn; demonstrates in vitro cytotoxicity against DU145 and K562 cells with IC50 of 100 and 15 nM; potently inhibits tumor growth in a variety of xenograft nude mouse models, does not exhibit hematotoxicity, liver damage, or neurotoxicity shows strong synergy with several chemotherapeutic agents.
H2244	Rigosertib	592542-59-1	Rigosertib (ON 01910) is a potent, non-ATP-competitive PLK1 inhibitor (IC50=9-10 nM), selectively induces mitotic G2/M arrest and apoptosis in cancer cells; also exhibits inhibitory activity against PDGFR, Abl, and Flt-1, at higher concentrations, inhibits CDK1, Plk2, Src, and Fyn; demonstrates in vitro cytotoxicity against DU145 and K562 cells with IC50 of 100 and 15 nM; potently inhibits tumor growth in a variety of xenograft nude mouse models, does not exhibit hematotoxicity, liver damage, or neurotoxicity shows strong synergy with several chemotherapeutic agents.
H2243	Poloxin-2	1807690-39-6	A potent, selective PLK1 PBD inhibitor with IC50 of 1.36 uM; shows >10-fold selectivity over Plk2 PBD and Plk3 PBD; significantly improved potency and selectivity over Poloxin; induces mitotic arrest and apoptosis in cultured human tumor cells at low micromolar concentrations.
H2242	Poloxin	321688-88-4	Poloxin is the first reported PLK1 PBD inhibitor with IC50 of 6.4 uM, shows less potent inhibition for Plk2 PBD and Plk3 PBD; inhibits the function of the Plk1 PBD in vitro, and cause Plk1 mislocalization, chromosome congression defects, mitotic arrest, and apoptosis in HeLa cells; activates the spindle assembly checkpoint and inhibits tumor growth in xenograft mouse models.
H2241	Poloxime	17302-61-3	An analog of thymoquinone that blocks pSer/pThr recognition by Plk1 Polo-box domain as a phosphate mimic.
H2240	Poloppin II	2248068-54-2	Poloppin II is an orally active, Poloppin derivative inhibitor of protein-protein interaction via the PBD of the mitotic Polo-like kinase (PLK) with IC50 of 41 uM in FP assays, exhibits IC50 of 61 nM cellular assay for mitotic arrest; is also active against PLK2 PDB with an IC50 of 105 uM in FP assay, engages PLK1 and PLK4, sensitizes cells expressing mutant KRAS by approximately 5-fold; demonstrates effectivity gainst KRAS-expressing cancer xenografts.
H2239	Poloppin	683808-78-8	Poloppin is a cell-active, small molecule inhibitor of protein-protein interaction via the Polo-box domain (PBD) of the mitotic Polo-like kinase (PLK) with IC50 of 26.9 uM (PLK1) in FP assays; triggers dose-dependent mitotic arrest with non-congressed chromosomes in human cell lines, preferentially kills cells expressing mutant KRAS (SW48 G12D GI50=5.2 uM, SW48 Wt GI50=13.7 uM), sensitizes mutant KRAS-expressing cells to clinical inhibitors of c-MET.

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