- 5-Fluorouridine is a metabolite of 5-fluorouracil with anticancer activity.
- Tz-Feng Lin, .et al. , Mater Today Commun, 2022, 33: 104284
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Topoisomerase inhibitor
Amonafide is a DNA intercalator and topoisomerase II inhibitor for the treatment of neoplastic diseases, one of Antitumor agent.
- Veronica Rendo, .et al. , Nat Commun, 2020, 11: 1308 PMID: 32161261
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HDAC3 inhibitor
RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM, exhibits > 200-fold selectivity over other HDAC.- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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Topoisomerase IV inhibitor
Ciprofloxacin Hydrochloride is a broad-spectrum antimicrobial carboxyfluoroquinoline, interfering with the bacterial DNA gyrase, inhibiting the DNA synthesis, and preventing bacterial cell growth.- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
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PARP1 inhibitor
AG14361 is a potent PARP inhibitor, enhanced TMZ cytotoxicity in MMR(mismatch repair)-proficient / deficient cells.- Vimal Pandey, .et al. , Scientific Reports, 2019, 9, Article number: 5012 PMID: 30899038
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Topoisomerase inhibitor
Idarubicin is an anthracycline antibiotic that is an anti-leukemia agent with higher DNA binding capacity and greater cytotoxicity than daunorubicin.- Wei Y, .et al. , Mol Cell, 2017, Jun 1;66(5):581-596.e6 PMID: 28552615
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PI3K inhibitor
Wortmannin is a potent, selective, cell-permeable and irreversible inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase) (IC50 = 2 - 4 nM) which also potently inhibits polo-like kinase 1 (PLK1) (IC50 = 5.8 nM).
- Weili Chen, .et al. , Communications Biology, 2024, 7:488
- Hirotake Ishida, .et al. , J Neurosci, 2021, Oct 13;41(41):8494-8507 PMID: 34452938
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PARP inhibitor
PJ 34 hydrochloride is a potent inhibitor of poly(ADP-ribose) polymerase (PARP) (EC50 = 20 nM).- Wigle TJ, .et al. , SLAS Discov, 2019, Dec 19:2472555219883623 PMID: 31855104
- Alvin Z.Lu, .et al. , Biochem Pharmacol, 2019, May 7. pii: S0006-2952(19)30171-6 PMID: 31075269
- Hoechst 33258 trihydrochloride is a cell dye for DNA quantitation.
- Xiao-Hong Guo, .et al. , Oncol Rep, 2021, Dec;46(6):253 PMID: 34643248
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Protein Synthesis Inhibitor
Cycloheximide (also known as actidione) is used as an selective antibiotic. It inhibits the protein synthesis (DNA-dependent RNA) of saprobic fungi eukaryotes. by binding with the 80S ribosome, while inactive against dermatophytes and systemic fungi.- Xiao-Yi Zhang, .et al. , Free Radic Biol Med, 2025, Aug 25:S0891-5849(25)00940-2 PMID: 40865778
- Wan-Cheng Liu, .et al. , Nat Commun, 2025, Jun 3;16(1):5154 PMID: 40461504
- Xingmei Shu, .et al. , Chin Med J (Engl), 2025, May 23 PMID: 40405358
- Jing Wang, .et al. , Mol Cell, 2025, May 15;85(10):1999-2016.e11 PMID: 40328247
- Yang Liao, .et al. , Cell Signal, 2025, Jul:131:111735 PMID: 40081551
- Xiangdong Qiu, .et al. , Cardiovascular Toxicology, 2025, 25: 427-440
- Tianfeng Huang, .et al. , Mol Neurobiol, 2024, Sep 13 PMID: 39271624
- Han Xiao, .et al. , JPA, 2023, Apr 19
- Shuanghui Lu, .et al. , Chem Biol Interact, 2022, Dec 1;368:110219 PMID: 36243147
- Ke Chen, .et al. , Cancer Commun (Lond), 2021, Apr; 41(4): 316-332 PMID: 33591636
- Zhiyuan Qin, .et al. , Cancers (Basel), 2021, Feb 4;13(4):618 PMID: 33557163
- Hua Xu, .et al. , Cancers (Basel), 2020, Apr; 12(4): 831 PMID: 32235588
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DNA topoisomerase II inhibitor
Beta-Lapachone is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase.- Xiaoling Li, .et al. , ACS Appl. Bio Mater, 2020, 3, 3, 1769-1778
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DNA/RNA Synthesis inhibitor
Clofarabine is a second generation purine nucleoside analog with antineoplastic activity- Xie J, .et al. , Pediatr Blood Cancer, 2019, Dec 25:e28133 PMID: 31876116
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Topoisomerase inhibitor
Epirubicin is a cell-permeable antitumor antibiotic. A stereoisomer of Doxorubicin that exhibits reduced cardiotoxicity. Epirubicin?€?s antitumor actions are mediated by targeting and inhibiting Topo II (topoisomerase II).- Xiu-wu Pan, .et al. , Oncol Rep, 2016, Jan;35(1):334-42 PMID: 26496799
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Selective SIRT2 inhibitor
SirReal2 is a potent and selective Sirt2 inhibitor with IC50 of 140 nM.- Yang Li, .et al. , Neoplasia, 2018, Jul; 20(7): 745-756 PMID: 29925042
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DNA/RNA Synthesis inhibitor
Oxaliplatin is a platinum-based antineoplastic agent that is used in cancer chemotherapy. In vivo studies showed that Oxaliplatin has anti-tumor activity against colon carcinoma through its (non-targeted) cytotoxic effects.- Yao-Yu Hsieh, .et al. , Mol Oncol, 2023, Oct 16 PMID: 37842807
- Mohamed Elbadawy, .et al. , Biomed Pharmacother, 2021, Oct;142:112043 PMID: 34411919
- Tatsuya Usui, .et al. , Int J Mol Sci, 2018, Apr; 19(4): 1098 PMID: 29642386
- Shimokawa M, .et al. , Nature, 2017, May 11;545(7653):187-192 PMID: 28355176
- Eri Takiguchi, .et al. , Exp Ther Med, 2017, Nov; 14(5): 4293-4299 PMID: 29067110
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ATM inhibitor
AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities.- Yi-Ru Pan, .et al. , Biomolecules, 2020, Nov 9;10(11):1529 PMID: 33182492
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DNA synthesis inhibitor
Gemcitabine (LY 188011) is a DNA synthesis inhibitor which inhibits the growth of BxPC-3, Mia Paca-2, PANC-1, PL-45 and AsPC-1 cells with IC50s of 37.6, 42.9, 92.7, 89.3 and 131.4 nM, respectively.- Yi-Ru Pan, .et al. , Int J Biol Sci, 2023, May 21;19(9):2772-2786 PMID: 37324940
- Khan Mohammad Imran, .et al. , Pharmaceutics, 2023, May 24;15(6):1585 PMID: 37376034
- Yi-Ru Pan, .et al. , Biomolecules, 2020, Nov 9;10(11):1529 PMID: 33182492
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ATM/ATR inhibitor
VE-821 is a potent and selective inhibitor of protein kinase ATR.- Yiovana Veronica Okraine, .et al. , Cell Death Dis, 2025, Jul 8;16(1):503 PMID: 40628724
- Atsushi Saito, .et al. , Cell Rep, 2023, May 30;42(5):112479 PMID: 37178686
- Mitsuru Sasaki-Honda, .et al. , Hum Mol Genet, 2018, Dec 1; 27(23): 4024-4035 PMID: 30107443
- Kim J, .et al. , Mol Cell, 2018, Jan 4;69(1):36-47.e7 PMID: 29249653
- Antonio Postigo, .et al. , Cell Rep, 2017, May 2; 19(5): 1022-1032 PMID: 28467896
- Nnennaya Kanu, .et al. , Genome Biol, 2016, 17: 185 PMID: 27634334
- Carolyn Botting, .et al. , Virol J, 2016, 13: 15 PMID: 26817608
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HDAC inhibitor
AR-42 is a novel HDAC inhibitor, exhibits biologic activity against malignant mast cell lines via down-regulation of constitutively activated Kit.- Yong-Hui Liao, .et al. , Mol Med Rep, 2018, Feb; 17(2): 2803-2810 PMID: 29257262
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DNA/RNA Synthesis inhibitor
Raltitrexed (Tomudex) is an inhibitor of thymidylate synthase and also is one of the strongest antimetabolites in use.- Yool Lee, .et al. , Sci Adv, 2021, 7
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PARP inhibitor
Olaparib (AZD2281) is an inhibitor of poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair.- Yuki Yoshino, .et al. , Biochem Biophys Res Commun, 2025, Jan:742:151153 PMID: 39672008
- Saptarshi Sinha, .et al. , Med Oncol, 2024, Jan 6;41(2):49 PMID: 38184505
- Erika Nakatsuka, .et al. , Transl Oncol, 2024, Sep 12:50:102119 PMID: 39270525
- Callum G Jones, .et al. , Cancers (Basel), 2024, Feb 21;16(5):863 PMID: 38473223
- Aurelie Vanderlinden, .et al. , Br J Cancer, 2023, Nov;129(11):1829-1840 PMID: 37777579
- Saptarshi Sinha, .et al. , Exp Cell Res, 2022, Nov 1;420(1):113338 PMID: 36075449
- Subhajit Chatterjee, .et al. , J Cancer Res Clin Oncol, 2022, Dec;148(12):3521-3535 PMID: 35962813
- Yuki Uchihara, .et al. , Mol Cell, 2022, Jul 21;82(14):2557-2570 PMID: 35594857
- Ji-Ye Kim, .et al. , Cell Death Dis, 2022, Mar 15;13(3):239 PMID: 35293383
- Emad Matanes, .et al. , Front Oncol, 2021, Oct 27;11:745981 PMID: 34778062
- Shino Endo, .et al. , Cancer Res Commun, 2021, 1(2): 90-105
- Yan Baglo, .et al. , Transl Oncol, 2021, Nov;14(11):101198 PMID: 34418731
- Joseph M Gozgit, .et al. , Cancer cell, 2021, Jul 22;S1535-6108(21)00340-8 PMID: 34375612
- Sefinew Molla, .et al. , DNA Repair (Amst), 2021, Jun 10;105:103157 PMID: 34144488
- Jianming Wang, .et al. , Cell Rep, 2021, Feb 16;34(7):108759 PMID: 33596418
- Ai Ito, .et al. , Biogerontology, 2021, Feb;22(1):119-131 PMID: 33216250
- Tim J Wigle, .et al. , Cell Chem Biol, 2020, Jul 16;27(7):877-887 PMID: 32679093
- Ali Divan, .et al. , Pharmacol Res Perspect, 2020, Apr; 8(2): e00586 PMID: 32342655
- Jianwei Dou, .et al. , J Sep Sci, 2020, Dec 4 PMID: 33275824
- Sai Dimple Manavitha Gullipalli, .et al. , Int. J. Adv. Pharm. Biotech, 2020, 6(2) 01-08
- Chao Zhang, .et al. , J Atheroscler Thromb, 2020, Sep 25 PMID: 32981917
- Wigle TJ, .et al. , SLAS Discov, 2019, Dec 19:2472555219883623 PMID: 31855104
- Wang Q, .et al. , Cancer Med, 2019, Dec 21 PMID: 31863638
- Molla S, .et al. , Pathol Oncol Res, 2019, Nov 25 PMID: 31768967
- Alvin Z.Lu, .et al. , Biochem Pharmacol, 2019, May 7. pii: S0006-2952(19)30171-6 PMID: 31075269
- Bian C, .et al. , Nat Commun, 2019, Feb 11;10(1):693 PMID: 30741937
- HC de Silva, .et al. , Cell Mol Life Sci, 2019, 1-16 PMID: 30725116
- Kamada Y, .et al. , Fitoterapia, 2018, Sep;129:94-101 PMID: 29928967
- 2018, .et al. , FEBS Open Bio, 2018, Jun; 8(6): 1001-1012 PMID: 29928579
- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Hiro Sato, .et al. , Nat Commun, 2017, 8: 1751 PMID: 29170499
- Charles-André Philip, .et al. , BMC Cancer, 2017, 17: 638 PMID: 28886696
- Rulina AV, .et al. , Cell Death Dis, 2016, Dec 1;7(12):e2505 PMID: 27906189
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DDX3 inhibitor
RK-33 is a potent and selective DDX3 inhibitor. RK-33 binds to DDX3 and abrogates its activity.- Zhang S, .et al. , Sci Rep, 2020, Jan 31;10(1):1557 PMID: 32005838
- Yang SNY, .et al. , Cells, 2020, Jan 9;9(1). PMID: 31936642
- NKP-1339 (IT-139) is the first-in-class ruthenium-based anticancer drug in clinical development against solid cancer with limited side effects.
- Zin Zin Ei, .et al. , Sci Rep, 2021, Nov 17;11(1):22448 PMID: 34789798
- Apaziquone is an indolequinone bioreductive prodrug and analog of mitomycin C with potential antineoplastic and radiosensitization activities.
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Topoisomerase I inhibitor
9-Aminocamptothecin is a topoisomerase I inhibitor with potent anticancer activity. -
HDAC inhibitor
Resminostat, also known as RAS2410, is a potent inhibitor of histone deacetylase (HDAC) classes I and II. It binds to and inhibits HDACs leading to an accumulation of highly acetylated histones. -
topoisomerase II inhibitor
Ametantrone (AM) is a synthetic 9,10-anthracenedione bearing two (hydroxyethylamino)ethylamino residues at positions 1 and 4 along with other anthraquinones and anthracyclines. -
HDAC4 inhibitor
Tasquinimod is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. - Fosteabine is an oral and prodrug analogue of cytarabine which is resistant to deoxycytidine deaminase.
- Palifosfamide is a synthetic mustard compound with potential antineoplastic activity.
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natural cyclic oligopeptide antibiotic
Antibiotic that inhibits bacterial protein synthesis. Inhibits mRNA-tRNA translocation by GTPase elongation factor G (EF-G), EF-TU(GTP)-catalyzed aa-tRNA delivery and the activity of initiation factor 2 (IF-2). Antitumor agent; induces cell cycle arrest and apoptosis in breast cancer cells via downregulation of FOXM1 expression. -
eIF4A3 inhibitor
eIF4A3-IN-1 (compound 53a) is a selective eukaryotic initiation factor 4A3 (eIF4A3) inhibitor (IC50=0.26 μM; Kd=0.043 μM).

