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Aurora A Kinase inhibitor
MLN8237（Alisertib）是一种选择性的Aurora A抑制剂，在无细胞试验中的IC50为1.2 nM。它对Aurora A的选择性比Aurora B高出200倍以上。目前处于第三阶段临床试验。- Shiang-Jie Yang, .et al. , Cell Death Dis, 2024, Jan 30;15(1):103 PMID: 38291041
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- Bucko PJ, .et al. , Elife, 2019, Dec 24;8. pii: e52220 PMID: 31872801
- Kimura M, .et al. , Exp Cell Res, 2018, Jun 1;367(1):73-80 PMID: 29571950
- Jing Wang, .et al. , J Cell Sci, 2017, Mar 15; 130(6): 1078-1093 PMID: 28167680
- Lessing D, .et al. , Proc Natl Acad Sci U S A, 2016, Dec 13;113(50):14366-14371 PMID: 28182563
- Jennifer M. Sahni, .et al. , J Biol Chem, 2016, Nov 4; 291(45): 23756-23768 PMID: 27650498
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CDK Inhibitor
AT7519 是一种多重周期蛋白依赖性激酶（CDKs）抑制剂，可能导致细胞周期阻滞、凋亡诱导以及抑制肿瘤细胞增殖。- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
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Aurora A Inhibitor
Aurora A Inhibitor I 是一种强效且选择性的 Aurora A 激酶 (AurA) 抑制剂，其 IC50 值为 3.4 nM（针对 Aurora A），并且对 Aurora B 具有极高的选择性，高达 1000 倍；这是一种有用的工具化合物，用于研究 Aurora A 激酶 在细胞中的作用。 -
Aurora Kinase B inhibitor
AZD 1152-HQPA 是一种高效且选择性的 Aurora B 抑制剂，其 Ki 值分别为 0.36 nM（Aurora B）和 1369 nM（Aurora A），并且相对于其他50种激酶具有高度的特异性。- Sakamoto K, .et al. , Leukemia, 2018, May 23 PMID: 29795241
- Jennifer M. Sahni, .et al. , J Biol Chem, 2016, Nov 4; 291(45): 23756-23768 PMID: 27650498
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PLK inhibitor
BI 2536 是一种选择性的 Plk1 抑制剂，能在低纳摩尔浓度下抑制 Plk1 酶的活性。- Ryuzaburo Yuki, .et al. , Eur J Pharmacol, 2024, Jan 15:963:176229 PMID: 38072041
- Nuria Gallisa-Sune, .et al. , Nat Commun, 2023, Apr 27;14(1):2434 PMID: 37105961
- Kei K Ito, .et al. , J Cell Biol, 2021, Mar 1;220(3):e202005153 PMID: 33492359
- Ryuzaburo Yuki, .et al. , J Cell Mol Med, 2021, Feb;25(3):1677-1687 PMID: 33465289
- Yamagishi A, .et al. , Int J Mol Sci, 2020, Feb 5;21(3) PMID: 32033461
- Bucko PJ, .et al. , Elife, 2019, Dec 24;8. pii: e52220 PMID: 31872801
- Watanabe K, .et al. , Nat Commun, 2019, Feb 25;10(1):931 PMID: 30804344
- Valérian Pasche, .et al. , Parasit Vectors, 2018, 11: 298 PMID: 29764454
- Takeshi Wakida, .et al. , eLife, 2017, 6: e29953 PMID: 29254517
- Majid Momeny, .et al. , Sci Rep, 2017, 7: 4204 PMID: 28646172
- Ifuji A, .et al. , Exp Cell Res, 2017, Nov 15;360(2):347-357 PMID: 28942021
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PLK Inhibitor
BI6727 是一种高效且选择性的 polo-like kinase (PLK) 1 抑制剂（酶 IC50 = 0.87 nM，EC50 = 11-37 nM，针对一系列癌症细胞系）。- Xiaofei Xin, .et al. , ACS Appl Mater Interfaces, 2019, 2019 PMID: 30933478
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ROCK inhibitor
Fasudil HCl 是一种环核苷酸依赖性蛋白激酶抑制剂和Rho相关激酶抑制剂（IC50 = 10.7 μM）。- Jiwan Choi, .et al. , Stem Cell Res Ther, 2024, Jul 29;15(1):229 PMID: 39075621
- Patrick D Lyden, .et al. , Sci Transl Med, 2023, Sep 20;15(714):eadg8656 PMID: 37729432
- Seongjun So, .et al. , Int J Mol Sci, 2022, Dec 31;24(1):701 PMID: 36614165
- Chengyu Xiang, .et al. , J Cardiovasc Transl Res, 2022, May 12 PMID: 35551627
- Yeonmi Lee, .et al. , Commun Biol, 2022, Jan 25;5(1):95 PMID: 35079104
- Jiwan Choi, .et al. , Stem Cell Res Ther, 2021, Nov 12;12(1):569
- Jee Myung Yang, .et al. , Exp Mol Med, 2021, Apr;53(4):631-642 PMID: 33828232
- Jooyoung Lee, .et al. , Cells, 2020, Jun; 9(6): 1521 PMID: 32580448
- Kumar M, .et al. , Behav Brain Res, 2018, Oct 1;351:4-16 PMID: 29807069
- Wei J, .et al. , Shock, 2018, Dec;50(6):706-713 PMID: 29283979
- Hofni A, .et al. , Naunyn Schmiedebergs Arch Pharmacol, 2017, Aug;390(8):801-811 PMID: 28493050
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CDK inhibitor
Flavopiridol（Alvocidib）是一种环依赖性激酶抑制剂，目前正在临床开发中，用于治疗慢性淋巴细胞性白血病。- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Zhiyuan Zhao, .et al. , J Biol Chem, 2017, Sep 15; 292(37): 15489-15500 PMID: 28743741
- Sami Kukkonen, .et al. , Retrovirology., 2014, 11: 30. PMID: 24742347
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ROCK Inhibitor
GSK429286A 是一种细胞渗透性、选择性的小分子抑制剂，专门针对 Rho-associated, coiled-coil containing protein kinase (ROCK)。 -
Aurora B Kinase inhibitor
Hesperadin 是一种针对人类 Aurora B 的抑制剂，其 IC50 值为 40 nM，用于防止底物的磷酸化。它显著降低了 AMPK、Lck、MKK1、MAPKAP-K1、CHK1 和 PHK 的活性，但在体内不抑制 MKK1 的活性。- Wenbin Ji, .et al. , PLoS One, 2016, 11(4): e0153518 PMID: 27082996
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PLK Inhibitor
HMN-214 抑制 polo-like 和 cyclin-dependent kinase 活性，具有强大的抗微管效果，并在广泛的人源异种移植瘤中引起深刻的凋亡和抗肿瘤活性。- Yao-Yu Hsieh, .et al. , Mol Oncol, 2023, Oct 16 PMID: 37842807
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CDK/Aurora A/B Inhibitor
JNJ-7706621 是一种广谱 CDK 抑制剂，在 CDK1/2 上具有最高的抑制活性，其 IC50 分别为 9 nM/4 nM，并且在无细胞试验中对 CDK1/2 的选择性比 CDK3/4/6 高出6倍以上。它还强效抑制 Aurora A/B，并且对 Plk1 和 Wee1 无活性。- Yuta Tanizaki, .et al. , Commun Biol, 2022, 5: 112 PMID: 35132135
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WEE1 Inhibitor
MK-1775 是一种在体外和体内都具有强效和选择性的 Wee1激酶抑制剂。- Hayden L Bell, .et al. , Cancer Cell Int, 2023, Sep 15;23(1):202 PMID: 37715172
- Chiao-Ping Chen, .et al. , Biomed Pharmacother, 2023, Oct:166:115389 PMID: 37659202
- Ting-Yu Chang, .et al. , Biomed Pharmacother, 2021, Jun;138:111485 PMID: 33740521
- 2018, .et al. , FEBS Open Bio, 2018, Jun; 8(6): 1001-1012 PMID: 29928579
- Rulina AV, .et al. , Cell Death Dis, 2016, Dec 1;7(12):e2505 PMID: 27906189
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PLK Inhibitor
ON-01910 对慢性淋巴细胞性白血病细胞具有选择性的细胞毒性，其作用机制涉及双重途径：PI3K/AKT抑制和氧化应激诱导。 -
CDK 4/6 inhibitor
PD 0332991 HCl 是一种口服可用的吡啶并嘧啶衍生的环依赖性激酶 (CDK) 抑制剂，具有潜在的抗肿瘤活性。- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Hiroki Ozawa, .et al. , Transl Oncol, 2022, Feb;16:101307 PMID: 34902741
- Cong Li, .et al. , Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Pirita Pekkonen, .et al. , Cell Cycle, 2014, Dec 1; 13(23): 3670-3684 PMID: 25483078
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Aurora inhibitor
PHA-680632 是一种强效的 Aurora A、Aurora B 和 Aurora C 抑制剂，其半抑制浓度（IC50）分别为 27 nM、135 nM 和 120 nM。相比之下，它对 FGFR1、FLT3、LCK、PLK1、STLK2 和 VEGFR2/3 的 IC50 高出 10 到 200 倍。 -
Aurora inhibitor
Danusertib (PHA-739358) 是一种针对 Aurora A/B/C 的 Aurora 激酶抑制剂，在无细胞试验中的 IC50 分别为 13 nM/79 nM/61 nM，对 Abl、TrkA、c-RET 和 FGFR1 有适度的抑制效力，对 Lck、VEGFR2/3、c-Kit、CDK2 等的抑制效力较低。目前处于临床试验第二阶段。- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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CDK Inhibitor
PHA-793887，一种新型的强效Cdk抑制剂，在低浓度下针对多种周期蛋白依赖性激酶，并对多种癌症细胞系表现出高活性。- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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CDK Inhibitor
Roscovitine（Seliciclib）是一种CDK抑制剂，它优先抑制包括CDK2、CDK7和CDK9在内的多个酶靶点。- Abdel-Aziz S Shatat, .et al. , Purinergic Signal, 2024, May 27 PMID: 38801618
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Vimal Pandey, .et al. , Scientific Reports, 2019, 9, Article number: 5012 PMID: 30899038
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CDK inhibitor
SNS-032 (BMS-387032) 是一种高度选择性且有效的环依赖性激酶（Cdks）2、7 和 9 的抑制剂，具有体外生长抑制效果，并能够在恶性 B 细胞中诱导凋亡。 -
Aurora inhibitor
SNS-314 Mesylate 是一种强效且选择性的 Aurora A、Aurora B 和 Aurora C 抑制剂，其半抑制浓度（IC50）分别为 9 nM、31 nM 和 3 nM。相比之下，它对 Trk A/B、Flt4、Fms、Axl、c-Raf 和 DDR2 的抑制作用较弱。目前处于临床试验第一阶段。 -
Aurora Kinase inhibitor
VX-680 是一种强效且选择性的小分子Aurora激酶抑制剂。- Helen E. Grimsley, .et al. , bioRxiv, 2024, Jan 23
- Sakamoto K, .et al. , Leukemia, 2018, May 23 PMID: 29795241
- W. Joost Lesterhuis, .et al. , Sci Rep, 2015, 5: 12298 PMID: 26193793
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ROCK Inhibitor
Y-27632 是一种 Rho-Associated Coil Kinase (ROCK) 抑制剂，能够提高人类胚胎干细胞（hESCs）的克隆效率。- Peilin Li, .et al. , Ecotoxicol Environ Saf, 2024, Dec:288:117330 PMID: 39571255
- Takaaki Fujimura, .et al. , NPJ Precis Oncol, 2024, Nov 17;8(1):264 PMID: 39551860
- Ayumi Horikawa, .et al. , In Vitro Cell Dev Biol Anim, 2024, Nov 15 PMID: 39546193
- Giovanni Tosi, .et al. , Nat Commun, 2024, Sep 18;15(1):8214 PMID: 39294175
- Christina Zarouchlioti, .et al. , EBioMedicine, 2024, Oct:108:105328 PMID: 39278108
- Kyunghyun Park, .et al. , Advanced Therapeutics, 2024, 7(6)
- Maude Hamilton, .et al. , Biol Open, 2024, Jan 15; 13(1): bio059919 PMID: 38252116
- Oliver Podmanicky, .et al. , Hum Mol Genet, 2024, Mar 1; 33(5): 435-447 PMID: 37975900
- Masayuki Fukumoto, .et al. , PLoS One, 2024, Dec 5;19(12):e0313312 PMID: 39636897
- Johannes Robert Fleischer, .et al. , Mol Cancer, 2023, Jan 24;22(1):17 PMID: 36691028
- Vignesh Jayarajan, .et al. , Cells, 2023, Jan 17;12(3):346 PMID: 36766688
- Giulia Bastianello, .et al. , Cell Rep, 2023, Dec 26;42(12):113555 PMID: 38088930
- Charlotte Phelps, .et al. , Sci Rep, 2023, Oct 23;13(1):18062 PMID: 37872186
- Mathilde Meyenberg, .et al. , Sci Rep, 2023, Aug 26;13(1):13964 PMID: 37633982
- Yu-Ting Wu, .et al. , J Biomed Sci, 2023, Aug 21;30(1):70 PMID: 37605213
- Heming Ning, .et al. , In Vitro Cell Dev Biol Anim, 2023, Jun;59(6):410-419 PMID: 37405627
- Eric Lian, .et al. , STAR Protoc, 2023, May 22;4(2):102314 PMID: 37220001
- Stephanie T Pohl, .et al. , Methods Mol Biol, 2023, 2584:371-387 PMID: 36495461
- Charlotte Phelps, .et al. , Am J Physiol Cell Physiol, 2023, Mar 1;324(3):C787-C797 PMID: 36689673
- Shunsuke Murakami, .et al. , Regen Ther, 2022, Nov 25;21:574-583 PMID: 36475025
- Sergio Pedraza-Arevalo, .et al. , STAR Protoc, 2022, Aug 30;3(3):101656 PMID: 36092820
- Ji-Hyun Lee, .et al. , Cell Stem Cell, 2022, May 5; 29(5): 826-839 PMID: 35523142
- Adam Pietrobon, .et al. , Cell Rep, 2022, Jul 5;40(1):111048 PMID: 35793620
- Sarkawt Hamad, .et al. , Stem Cell Res Ther, 2022, Jun 11;13(1):251 PMID: 35690874
- Stasia Krishtul, .et al. , Polym Adv Technol, 2022, 33( 11): 3842-3852
- Peter T Ruane, .et al. , Hum Reprod, 2022, Apr 1;37(4):777-792 PMID: 35079788
- Takayuki Miyoshi, .et al. , J Gastroenterol, 2022, Jun;57(6):441-452 PMID: 35294680
- Ana-Maria Cujba, .et al. , Cell Rep, 2022, Mar 1;38(9):110425 PMID: 35235779
- Dan Zhao, .et al. , Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
- Antigoni Gogolou, .et al. , Curr Protoc, 2021, Jun;1(6):e137 PMID: 34102038
- Tiago De Oliveira, .et al. , Cancers (Basel), 2021, Mar 2;S2451-9456(21)00095-7 PMID: 33671096
- Denise Muller, .et al. , BMC Med, 2021, Nov 16;19(1):300 PMID: 34781947
- Ayumi Horikawa, .et al. , PloS one, 2021, Jul 12;16(7):e0254373 PMID: 34252142
- Hayato Mizuta, .et al. , Nat Commun, 2021, Feb 24;12(1):1261 PMID: 33627640
- Scott Bell, .et al. , Stem Cell Reports, 2021, Jul 13;16(7):1749-1762 PMID: 34214487
- Shenyang Li, .et al. , J Cell Mol Med, 2020, Dec 20;25(2):1207-1220 PMID: 33342057
- Takao FUCHIGAMI, .et al. , J Appl Oral Sci, 2020, 28: e20190558 PMID: 32348439
- Jing-Yu Lin, .et al. , Cell Discov, 2020, 6: 20 PMID: 32284878
- Yu Huang, .et al. , Stem Cells Int, 2019, 2019: 3975689 PMID: 31565060
- XinYan, .et al. , Stem Cell Res, 2019, May 17 PMID: 31141763
- Daniela F. Duarte Campos, .et al. , J Biomed Mater Res A, 2019, April 22 PMID: 31012205
- Scott Bell, .et al. , Am J Hum Genet, 2019, May 2;104(5):815-834 PMID: 31031012
- Ooi J, .et al. , Cell Rep, 2019, Feb 26;26(9):2494-2508 PMID: 30811996
- Scott Bell, .et al. , Stem Cell Reports, 2018, Jul 10; 11(1):183-196 PMID: 29937144
- Christina Zarouchlioti, .et al. , Am J Hum Genet, 2018, Apr 5; 102(4): 528-539 PMID: 29526280
- Ai Takemoto, .et al. , Sci Rep, 2017, 7: 42186 PMID: 28176852
- Scott Bell, .et al. , Stem Cells Transl Med, 2017, Mar; 6(3): 886-896 PMID: 28170165
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osteoclastic bone resorption inhibitor
Zoledronic acid is a bisphosphonate used for the treatment of multiple myeloma and prostate cancer. -
Akt inhibitor
A-674563 是一种 B/Akt 抑制剂，其 IC50 为 14 nM，同时也显示出对 PKA 和 CDK2 的抑制活性，其 IC50 分别为 16 nM 和 46 nM。- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Kobayashi T, .et al. , Biochem Biophys Res Commun, 2018, Jan 1;495(1):1468-1475 PMID: 29196261
- Lin Xu, .et al. , Biochem Biophys Res Commun, 2016, Apr 15;472(4):662-8 PMID: 26920060
- Zou Y, .et al. , Biochem Biophys Res Commun, 2016, Aug 12;477(1):1-8 PMID: 26970307
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Chk inhibitor
LY2603618 是一种 chk2 抑制剂，它通过结合并抑制 chk2 的活性，可能阻止由 DNA 损伤剂引起的 DNA 修复。- Hayakawa K, .et al. , Biochem Biophys Res Commun, 2018, Dec 2;506(4):983-989 PMID: 30404732
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CDK Inhibitor
Dinaciclib (SCH 727965) 是一种强效且选择性的环依赖性激酶（CDK）抑制剂，选择性抑制 CDK1、CDK2、CDK5 和 CDK9，其 IC50 值分别为 3、1、1 和 4 nM。- Vineeta Teotia, .et al. , ACS Omega, 2024, Sep 13;9(38):39873-39892 PMID: 39346877
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- Sepideh Izadi, .et al. , Pharm Res, 2020, Sep 17;37(10):196 PMID: 32944844
- Shahin Hallaj, .et al. , Life Sci, 2020, Jul 26 PMID: 32726663
- Washio I, .et al. , Drug Metab Dispos, 2018, Mar;46(3):214-222 PMID: 29246888
