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SBE13

Catalog No. A21696
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Plk1 inhibitor

SBE13 is a potent and selective Plk1 inhibitor, with an IC50 of 200 pM; SBE13 poorly inhibits Plk2 (IC50>66?μM) or Plk3 (IC50=875?nM). 了解更多

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TAK-960 hydrochloride

Catalog No. A21703
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PLK1 inhibitor

TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM at 10 μM ATP; TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. 了解更多

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LY2603618 (IC-83)

Catalog No. A11036
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Chk 抑制剂

LY2603618 (IC-83)是一种chk2抑制剂，可与chk2结合并抑制其活性，这可能会阻止DNA损伤剂引起的DNA修复。了解更多

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- Hayakawa K, .et al. Planar compression of extracellular substrates induces S phase arrest via ATM-independent CHK2 activation, Biochem Biophys Res Commun, 2018, Dec 2;506(4):983-989 PMID: 30404732
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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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SCH 900776 (MK-8776)

Catalog No. A11167
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Chk1 抑制剂

SCH 900776 (MK-8776)是靶向细胞周期检查点激酶1（Chk1）的药物，无细胞试验中IC50为3 nM，比作用于Chk2选择性高500倍。具有潜在的放射增敏和化学增敏活性。了解更多

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- Hong Yang, .et al. APOBEC3B Improves Response to PD-1 Blockade Through DSBs-ATR-CHK1 Pathway, Research Square, 2022, May 9th
- Motofumi Suzuki, .et al. Radiation-Induced Autophagy in Human Pancreatic Cancer Cells is Critically Dependent on G2 Checkpoint Activation: A Mechanism of Radioresistance in Pancreatic Cancer, Int J Radiat Oncol Biol Phys, 2021, May 25;S0360-3016(21)00361-8 PMID: 34112559
- Min Wu, .et al. FLT3/ITD Cooperates With Rac1 To Modulate The Sensitivity Of Leukemic Cells To Chemotherapeutic Agents Via Regulation Of DNA Repair Pathways, Haematologica, 2019, 104 PMID: 30975911
- Permata TBM, .et al. Base excision repair regulates PD-L1 expression in cancer cells, Oncogene, 2019, Feb 12 PMID: 30755733
- Hiro Sato, .et al. DNA double-strand break repair pathway regulates PD-L1 expression in cancer cells, Nat Commun, 2017, 8: 1751 PMID: 29170499
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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

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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