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Aurora A Kinase inhibitor
MLN8237 (Alisertib) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Phase 3..- 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 is an inhibitor of multiple cyclin-dependent kinases (CDKs), which may result in cell cycle arrest, induction of apoptosis, and inhibition of tumor cell proliferation.- 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 is a potent and selective inhibitor of Aurora A kinase (AurA), with IC50 values to be 3.4 nM (Aurora A) and unusually high selectivity 1000 fold against Aurora B; a useful tool compound for investigating the cellular role of Aurora A kinases.
- Azathioprine is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.
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Aurora Kinase B inhibitor
AZD 1152-HQPA is a highly potent and selective inhibitor of Aurora B, with Ki values to be 0.36 (Aurora B) and 1369 nM (Aurora A) respectively and has a high specificity versus a panel of 50 other kinases.- 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 is a selective inhibitor of Plk1, which inhibits Plk1 enzyme activity at low nanomolar concentrations.- 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 is a highly potent and selective polo-like kinase (PLK) 1 inhibitor (enzyme IC50 = 0.87 nM, EC50 = 11-37 nM on a panel of cancer cell lines).- Xiaofei Xin, .et al. , ACS Appl Mater Interfaces, 2019, 2019 PMID: 30933478
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Aurora Inhibitor
CCT129202 is a representative of a structurally novel series of imidazopyridine small-molecule inhibitors of Aurora kinase activity. It shows high selectivity for the Aurora kinases over a panel of other kinases tested and inhibits proliferation in multiple cultured human tumor cell lines.
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ROCK inhibitor
Fasudil HCl is a cyclic nucleotide-dependent protein kinase inhibitor and Rho-associated kinase inhibitor (IC50 = 10.7 μM).- 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) is a cyclin-dependent kinase inhibitor under clinical development for the treatment of chronic lymphocytic leukemia.- 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 is a cell-permeable, selective small molecule inhibitor of Rho-associated, coiled-coil containing protein kinase (ROCK). -
Aurora B Kinase inhibitor
Hesperadin is a human Aurora B inhibitor with an IC50 of 40 nM for the prevention of the phosphorylation of substrate. It markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1 and PHK while it does not inhibit MKK1 activity in vivo.- Wenbin Ji, .et al. , PLoS One, 2016, 11(4): e0153518 PMID: 27082996
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PLK Inhibitor
HMN-214 inhibits polo-like and cyclin-dependent kinase activity, has potent antimicrotubular effects and results in profound apoptosis and antitumor activity in a broad spectrum of human xenografts.- Yao-Yu Hsieh, .et al. , Mol Oncol, 2023, Oct 16 PMID: 37842807
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CDK/Aurora A/B Inhibitor
JNJ-7706621 is pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.- Yuta Tanizaki, .et al. , Commun Biol, 2022, 5: 112 PMID: 35132135
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WEE1 Inhibitor
MK-1775 is a potent and selective Wee1 kinase inhibitor in vitro and in vivo.- 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 is selectively cytotoxic for chronic lymphocytic leukemia cells through a dual mechanism of action involving PI3K/AKT inhibition and induction of oxidative stress. -
CDK 4/6 inhibitor
PD 0332991 HCl is an orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity.- 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 is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively. It has 10- to 200-fold higher IC50 for FGFR1, FLT3, LCK, PLK1, STLK2, and VEGFR2/3. -
Aurora inhibitor
Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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CDK Inhibitor
PHA-793887, a novel potent inhibitor of Cdk, target on kinds of cyclin-dependent kinase under low concentrations and poses high activity against several cancer cell lines.- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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CDK Inhibitor
Roscovitine (Seliciclib) is a CDK inhibitor that preferentially inhibit multiple enzyme targets including CDK2, CDK7 and CDK9.- 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) is a highly selective and potent inhibitor of cyclin-dependent kinases (Cdks) 2, 7, and 9, with in vitro growth inhibitory effects and ability to induce apoptosis in malignant B cells. -
ROCK inhibitor
Thiazovivin is a selective inhibitor of Rho-associated kinase (ROCK). -
Aurora Kinase inhibitor
VX-680 is a potent and selective small-molecule inhibitor of the Aurora kinases.- 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 is a Rho-Associated Coil Kinase (ROCK) inhibitor that increases the cloning efficiency of human embryonic stem cells (hESCs).- 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
- 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 which used to multiple myeloma and prostate cancer treament. -
Akt inhibitor
A-674563 is a B/Akt inhibitor with an IC50 of 14 nM and also shows inhibitory activity against PKA and CDK2 with IC50 of 16 and 46 nM, respectively.- 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 is a chk2 inhibitor that binds to and inhibits the activity of chk2, which may prevent the repair of DNA caused by DNA-damaging agents.- Hayakawa K, .et al. , Biochem Biophys Res Commun, 2018, Dec 2;506(4):983-989 PMID: 30404732
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CDK inhibitor
Flavopiridol HCl is an inhibitor of cyclin-dependent kinases. The (-)-cis form induces apoptosis in particular tumor cells. -
CDK Inhibitor
PHA-848125 (Milciclib) is an orally bioavailable inhibitor of CDKs and TRKA with potential antineoplastic activity. -
CDK Inhibitor
Dinaciclib (SCH 727965) is a potent and selective cyclin-dependent kinase (CDK) inhibitor, selectively inhibiting CDK1, CDK2, CDK5 and CDK9 with IC50 values of 3, 1, 1 and 4 nM respectively.- 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