SBE 13 HCl

製品コードS7720 バッチS772001

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₄H₂₈Cl₂N₂O₄
	分子量	479.4	CAS No.	1052532-15-6
Solubility (25°C)*	体外	DMSO	95 mg/mL (198.16 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	SBE 13 HCl is a potent and selective PLK1 inhibitor with IC50 of 200 pM, >4000-fold selectivity over Aurora A kinase, Plk2 and Plk3.
in vitro	SBE 13 decreases cell proliferation in various cancer cell lines, and causes a G2/M arrest followed by apoptosis. ^[1] In primary cells, SBE 13 does not impair cell cycle and thus proliferation of primary cells. ^[2] SBE13 in combination with Enzastaurin displays a synergistic reduction of cell proliferation and enhanced apoptosis induction in HCT116(p53-/-) cells. ^[3]

プロトコル(参考用のみ)

キナーゼアッセイ	Kinase assays
キナーゼアッセイ	To assay Plk1 and Aurora A kinase activity, cells are lysed after 13 hrs release in the presence of SBE13 after double thymidine block, and kinases are immunoprecipitated from lysates using antibodies as described. In brief, for each immunoprecipitation 800 µg of total protein were incubated with 1.5 µg Plk1 antibody cocktail, 3 µg Plk2 antibody, 3 µg Plk3 antibody, or 5 µg Aurora A antibody, respectively, for 2 hrs at 4°C on a rotator. Immunoprecipitated protein is collected using Protein G Agarose beads. The Plk1, Plk2 and Plk3 immunoprecipitates are incubated with 1 µg casein and with 1 µCi of [γ³²-P]ATP for 30 min at 37°C in kinase buffer. The Aurora A immunoprecipitates are incubated with 0.5 µl Histone and with 1 µCi of [γ³²-P]ATP for 60 min at room temperature in kinase buffer. Products from the kinase assays are fractionated on 10% Bis-Tris-polyacrylamide gels, and the phosphorylated substrate is visualized by autoradiography after an exposure of 12 to 36 hrs. An equal amount of immunoprecipitates is subjected to western blot analysis to confirm equal loading of Plk1, Plk2, Plk3 or Aurora A protein in kinase reactions. Immunoprecipitated Plk1 after 13 hrs release in the presence of SBE13 is assayed after de-phosphorylation using λ protein phosphatase and compared to kinase activity of endogenous immunoprecipitated Plk1. Activity of Plk1 kinase with and wiiiuithout de-phosphorylation is compared and the ratio between de-phosphorylated and “normal” endogenous immunoprecipitated Plk1 kinase activity is calculated.
細胞アッセイ	細胞株	HeLa, A431, HCT-15, HT-29, MCF-7, U2OS, LN-229, SKW 6.4, PC-3, Det-562, SK-BR-3, SK-OV-3 and A549nb cells
	濃度	100 μM
	反応時間	72 hours
	実験の流れ	Cells are treated with SBE13 one day after subculturing. Control cells are incubated with normal culture medium. Concentrations of SBE13 ranged from 1 nM–100 µM. The growth rate of 1 x 10⁵ cells per 6-well is determined by counting cells at 24, 48 and 72 hours after treatment. Cell culture studies are performed in triplicate for each time point.

参考

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

PLK1 inhibition dampens NLRP3 inflammasome-elicited response in inflammatory disease models [ J Clin Invest, 2023, 133(21)e162129]	PubMed: 37698938
PLK1 inhibition dampens NLRP3 inflammasome-elicited response in inflammatory disease models [ J Clin Invest, 2023, 133(21)e162129]	PubMed: 37698938
Inhibition of polo-like kinase 1 (PLK1) facilitates reactivation of gamma-herpesviruses and their elimination [ PLoS Pathog, 2021, 17(7):e1009764]	PubMed: 34297745
Effects of Aurora kinase A on mouse decidualization via Stat3-plk1-cdk1 pathway [ Reprod Biol Endocrinol, 2021, 19(1):162]	PubMed: 34715887
Inhibition of Polo-like kinase 1 (PLK1) facilitates the elimination of HIV-1 viral reservoirs in CD4 + T cells ex vivo [ Sci Adv, 2020, 6(29):eaba1941]	PubMed: 32832623
SF3B1 deficiency impairs human erythropoiesis via activation of p53 pathway: implications for understanding of ineffective erythropoiesis in MDS [ J Hematol Oncol, 2018, 11(1):19]	PubMed: 29433555
SF3B1 deficiency impairs human erythropoiesis via activation of p53 pathway: implications for understanding of ineffective erythropoiesis in MDS [ J Hematol Oncol, 2018, 11(1):19]	PubMed: 29433555

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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