PLK

Inhibitory Selectivity

Catalog No.	Inhibitor Name	PLK1	PLK2	PLK3	Other
A10134	BI 2536	****	**	**	PI3Kα,Met,Tie-2
A10135	Volasertib	****
A10673	Rigosertib	**
A10442	GSK461364	***
A12429	MLN0905	***
A13245	Ro3280	**
A14426	SBE 13 HCl	****		*
A13045	NMS-P937	***
A10452	HMN-214
A11146	TAK-960	****	**	*
A11438	GW843682X	***		**

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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BI 2536

Catalog No. A10134
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PLK 抑制剂

BI 2536是Plk1的选择性抑制剂，可在低纳摩尔浓度下抑制Plk1酶的活性。了解更多

Product Citations (9)

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- Kei K Ito, .et al. Cep57 and Cep57L1 maintain centriole engagement in interphase to ensure centriole duplication cycle, J Cell Biol, 2021, Mar 1;220(3):e202005153 PMID: 33492359
- Ryuzaburo Yuki, .et al. The tyrosine kinase v-Src modifies cytotoxicities of anticancer drugs targeting cell division, J Cell Mol Med, 2021, Feb;25(3):1677-1687 PMID: 33465289
- Yamagishi A, .et al. Targeting Insulin-Like Growth Factor 1 Receptor Delays M-Phase Progression and Synergizes with Aurora B Inhibition to Suppress Cell Proliferation, Int J Mol Sci, 2020, Feb 5;21(3) PMID: 32033461
- Bucko PJ, .et al. Subcellular drug targeting illuminates local kinase action, Elife, 2019, Dec 24;8. pii: e52220 PMID: 31872801
- Watanabe K, .et al. The Cep57-pericentrin module organizes PCM expansion and centriole engagement, Nat Commun, 2019, Feb 25;10(1):931 PMID: 30804344
- Valérian Pasche, .et al. Screening a repurposing library, the Medicines for Malaria Venture Stasis Box, against Schistosoma mansoni, Parasit Vectors, 2018, 11: 298 PMID: 29764454
- Takeshi Wakida, .et al. The CDK-PLK1 axis targets the DNA damage checkpoint sensor protein RAD9 to promote cell proliferation and tolerance to genotoxic stress, eLife, 2017, 6: e29953 PMID: 29254517
- Majid Momeny, .et al. Dacomitinib, a pan-inhibitor of ErbB receptors, suppresses growth and invasive capacity of chemoresistant ovarian carcinoma cells, Sci Rep, 2017, 7: 4204 PMID: 28646172
- Ifuji A, .et al. A novel immunofluorescence method to visualize microtubules in the antiparallel overlaps of microtubule-plus ends in the anaphase and telophase midzone, Exp Cell Res, 2017, Nov 15;360(2):347-357 PMID: 28942021
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BI6727 (Volasertib)

Catalog No. A10135
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PLK 抑制剂

BI6727 (Volasertib)是一种高效且选择性的polo样激酶（PLK）1抑制剂（在一组癌细胞系中，酶IC50 = 0.87 nM，EC50 = 11-37 nM）。了解更多

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- Xiaofei Xin, .et al. ROS responsive polymeric micelles for triggered simultaneous delivery of PLK1 inhibitor/miR-34a and effective synergistic therapy in pancreatic cancer, ACS Appl Mater Interfaces, 2019, 2019
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GW843682X

Catalog No. A11438
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PLK1/PLK3 抑制剂

GW843682X是polo-like激酶1（PLK1）和polo-like激酶3（PLK3）的选择性抑制剂（IC50值分别为2.2和9.1 nM）。了解更多

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- Kanada F, .et al. Histone acetyltransferase and Polo-like kinase 3 inhibitors prevent rat galactose-induced cataract, Sci Rep, 2019, Dec 27;9(1):20085 PMID: 31882756
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GSK461364

Catalog No. A10442
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PLK 抑制剂

GSK461364 是polo样激酶1 (Plk1)的ATP竞争性抑制剂。了解更多

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HMN-214

Catalog No. A10452
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PLK 抑制剂

HMN-214抑制polo样和细胞周期蛋白依赖性激酶活性，具有强有力的抗微管作用，并在广泛的人类异种移植物中导致深度凋亡和抗肿瘤活性。了解更多

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TAK-960

Catalog No. A11146
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PLK1 抑制剂?

TAK-960是新型的，口服可用的polo样激酶1选择性抑制剂，具有广谱的临床前抗肿瘤活性。了解更多

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ON-01910 (rigosertib)

Catalog No. A10673
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PLK 抑制剂

ON-01910 (rigosertib)通过涉及PI3K/AKT抑制和氧化应激诱导的双重作用机制对慢性淋巴细胞白血病细胞具有选择性的细胞毒性。了解更多

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MLN 0905

Catalog No. A12429
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PLK1 抑制剂

MLN0905是有效的选择性小分子PLK1抑制剂。MLN0905抑制包括DLBCL细胞系在内的多种人类肿瘤细胞的细胞增殖。了解更多

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RO3280

Catalog No. A13245
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PLK1 抑制剂

RO3280是一种有效的，高选择性的Polo样激酶1（PLK1）抑制剂，IC50为3 nM。了解更多

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NMS-1286937

Catalog No. A13045
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PLK 抑制剂

NMS-1286937是一种小分子Polo样激酶1（PLK1）抑制剂，具有潜在的抗肿瘤活性。了解更多

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SBE 13 HCl

Catalog No. A14426
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PLK 抑制剂

SBE 13 HCl是PLK1的选择性抑制剂，对于PLK1，PLK3和PLK2，IC 50值分别为200pM，875nM和66μM。了解更多

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LFM-A13

Catalog No. A16261
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BTK 抑制剂

LFM-A13是有效且选择性的Btk抑制剂，IC50为17.2 uM；也抑制PLK3，IC50为7.2 uM。了解更多

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AAPK-25

Catalog No. A19085
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Aurora/PLK dual 抑制剂

AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3Ser10 phosphorylation and followed by a surge in apoptosis. 了解更多

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Poloxime

Catalog No. A12145
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PLK1 inhibitor

Poloxime, a hydrolysis product of poloxin, is a non-ATP-competitive Plk1 inhibitor, with moderate Plk1 inhibitory activity. 了解更多

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