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DNA/RNA Synthesis inhibitor
Cidofovir (Vistide) is an antiviral used for the treatment of cytomegalovirus (CMV) infection (ie: retinitis).- Adhikary A, .et al. , J Phys Chem B, 2015, Sep 3;119(35):11496-505 PMID: 26237072
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eIF4E/eIF4G inhibitor
4EGI-1 is a competitive eIF4E/eIF4G interaction inhibitor by binding to eIF4E with KD of 25 uM.- Amnon Wittenstein, .et al. , PLoS Biol, 2023, Nov 9;21(11):e3002355 PMID: 37943958
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DNA/RNA Synthesis inhibitor
Daptomycin is a lipopeptide antibiotic used in the treatment of certain infections caused by Gram-positive organisms.- Carly Deusenbery, .et al. , ACS Infect Dis, 2023, Oct 13;9(10):1949-1963 PMID: 37646612
- Viktoria Lazar, .et al. , Nature, 2022, 610: 540-546 PMID: 36198788
- Shigeru Fujimura, .et al. , J Infect Chemother., 2015, Oct;21(10):756-9 PMID: 26162777
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DNA/RNA Synthesis inhibitor
Gemcitabine (Gemzar) is a newer chemotherapy drug acting by replacing one of the building blocks of nucleic acids during DNA replication in cancer cells, preventing tumor growth.- Chiao-Ping Chen, .et al. , Biomed Pharmacother, 2023, Oct:166:115389 PMID: 37659202
- G. R. Iglesias, .et al. , Polymers, 2018, 10(3), 269 PMID: 30966304
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RHA inhibitor
YK 4-279 is an inhibitor of RNA Helicase A (RHA) binding to the oncogenic transciption factor EWS-FLI1.- Christopher M Schafer, .et al. , Proc Natl Acad Sci U S A, 2020, Oct 20;117(42):26494-26502 PMID: 33020273
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DNA/RNA Synthesis inhibitor
Bleomycin sulfate is a mixture of the sulfate salts of basic glycopeptide antineoplastic antibiotics isolated from Streptomyces verticillus.- Daiheon Lee, .et al. , Drug Deliv Transl Res, 2025, Sep 26 PMID: 41004077
- Arina Morozan, .et al. , Sci Rep, 2023, Nov 23;13(1):20577 PMID: 37996447
- Mai Kanemaru, .et al. , J Dermatol Sci, 2018, Jan;93(1):41-49 PMID: 30655107
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DNA/RNA Synthesis inhibitor
CX-5461 is a first-in-class non-genotoxic small molecule targeted inhibitor of RNA polymerase I (Pol I) that activates the p53 pathway without causing DNA damage. It inhibits RNA polymerase I-driven transcription of rRNA with IC50s of 142, 113, and 54 nM in HCT-116, A375, and MIA PaCa-2 cells, respectively
- Hang Lin, .et al. , Commun Biol, 2024, Aug 9;7(1):963 PMID: 39122837
- Saruul Tungalag, .et al. , Int J Hematol, 2023, Feb 13 PMID: 36780110
- Martine Chebrout, .et al. , J Cell Sci, 2022, 135 (6): jcs258798 PMID: 35048992
- Taro Mannena, .et al. , Mol Biol Cell, 2021, 32:ar33, 1-11 PMID: 34495685
- Shuichiro Okamoto, .et al. , Biosci Biotechnol Biochem, 2020, Aug 15;1-8 PMID: 32799625
- Ahmed Abdullah Ahmed, .et al. , Sci Rep, 2020, 10: 12192 PMID: 32699225
- Abed Saady, .et al. , Dyes Pigm, 2020, 174: 107986
- Jackobel AJ, .et al. , Biochim Biophys Acta Gene Regul Mech, 2019, Aug 2:194408 PMID: 31382053
- Hiroaki Suzuki, .et al. , Cell Death Dis, 2018, Oct; 9(10): 975 PMID: 30250194
- Anastasia Gelgor, .et al. , Oncotarget, 2018, Mar 2; 9(17): 13822-13833 PMID: 29568397
- Wang ZF, .et al. , Cell Chem Biol, 2018, Nov 29. pii: S2451-9456(18)30378-7 PMID: 30503283
- Yuko Fujiwara, .et al. , EBioMedicine, 2018, Jul; 33: 33-48 PMID: 30049386
- Maïmouna Coura Kone, .et al. , Biol Reprod, 2016, Apr;94(4):95, 1-12 PMID: 26984997
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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.- Jian Gu, .et al. , Cell, 2026, Jan 22;189(2):418-434 PMID: 41448182
- 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 PMID: 37440912
- 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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IMPDH inhibitor
AVN-944 (also known as VX-944) serves as an effective oral inhibitor, specifically targeting and inhibiting IMPDH (inosine monophosphate dehydrogenase). This enzyme plays a crucial role as a rate-limiting factor in the synthesis of guanine nucleotides from scratch. Additionally, AVN-944 acts against the synthesis of RNA in arenaviruses, effectively preventing arenavirus infections. Demonstrating a wide spectrum of anti-cancer properties, AVN-944 is utilized in research related to multiple myeloma (MM) and acute myeloid leukemia (AML).
- Kevin Chiem, .et al. , Microbiol Spectr, 2023, Aug 17;11(4):e0474522 PMID: PMC10434227
- Desarey Morales Vasquez, .et al. , Viruses, 2020, Sep; 12(9): 1041 PMID: 32961956
- Park JG, .et al. , J Virol, 2020, Mar 17;94(7) PMID: 31941776
- Dunham EC, .et al. , Antiviral Res, 2018, Sep;157:140-150 PMID: 30031760
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DNA and RNA synthesis inhibitor
Fluorouracil (Adrucil) is a suicide inhibitor and works through irreversible inhibition of thymidylate synthase.- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Adi Jacob Berger, .et al. , Nat Cancer, 2021, 2, 1055-1070 PMID: 35121883
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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.- Sheng-Hsuan Lin, .et al. , Cancer Gene Therapy, 2026, 33, 289-300 PMID: 41654591
- 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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DNA/RNA Synthesis inhibitor
Tegafur is a chemotherapeutic 5-FU prodrug used in the treatment of cancers. It is a component of tegafur-uracil.- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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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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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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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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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 PMID: 33579708
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DNA synthesis inhibitor
Mitomycin C is a DNA crosslinking agent that inhibits DNA synthesis and induces apoptosis in a variety of cells.- Zhang H, .et al. , Cancer Commun, 2026, 46:Article 0028 PMID: 42147354
- Clement J F Heymann, .et al. , Res Sq, 2025, Nov 24:rs.3.rs-8051355 PMID: 41356367
- John A. Quinlan, .et al. , Advanced Nano Biomed, 2024, Sep 28 PMID: 41551720
- Gehlen-Breitbach S, .et al. , Int J Oral Sci, 2023, 15(1):16 PMID: 37024457
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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
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DNA/RNA Synthesis inhibitor
Floxuridine is an oncology drug that belongs to the class known as antimetabolites. -
nudix hydrolase family inhibitor
TH588 hydrochloride is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC50= 5 nM). -
DNA replication inhibitor
Enocitabine is a nucleoside analog, and is a potent DNA replication inhibitor, and a DNA chain terminator. -
RdRp inhibitor
Galidesivir hydrochloride (BCX 4430 hydrochloride) is a viral RNA-dependent RNA polymerase (RdRp) inhibitor; demonstrated broad-spectrum activity in multiple viruses and a favorable preliminary preclinical safety profile. -
DNA synthesis inhibitor
Thiarabine (OSI-7836) shows potent anti-tumor activity and inhibition of DNA synthesis. -
RAD51 inhibitor
Bractoppin is a potent and selective inhibitor of phosphopeptide recognition by the BRCA1 tBRCT domain. -
Pre-mRNA Splicing Inhibitor
Herboxidiene (GEX1A) is a potent phytotoxic polyketide from Streptomyces sp. A7847 with a diverse range of activities, including herbicidal, anti-cholesterol, anti-tumor effects. Herboxidiene inhibits the pre-mRNA splicing process by binding to spliceosome-associated protein (SAP) 155, a subunit of SF3b, in the splicesome. -
DNA polymerase theta (Polθ) inhibitor
RP-6685 is a potent, selective, and orally active inhibitor of DNA polymerase theta (Polθ), with an IC50 of 5.8 nM as measured by the PicoGreen assay. It exhibits significant antitumor efficacy in mouse xenograft models. Additionally, RP-6685 contains an alkyne functional group, making it a useful click chemistry reagent capable of undergoing copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules, enabling its application in chemical biology and drug discovery research. -
DHX9 inhibitor
ATX968 (example 31) is an orally active, potent, and selective inhibitor of ATP-dependent RNA helicase A (DHX9), with an EC50 of 0.054 μM in circBRIP1-expressing models. It demonstrates robust and durable tumor growth inhibition or regression in mouse xenograft studies using microsatellite instability-high (MSI-H) and mismatch repair-deficient (dMMR) colorectal cancer cell lines, highlighting its potential for targeted cancer therapy. -
Polθ DNA polymerase inhibitor
ART899 is a highly specific allosteric inhibitor of the DNA polymerase domain of polymerase theta (Polθ). It effectively enhances the radiosensitivity of tumor cells and demonstrates good tolerability when combined with fractionated radiation therapy. ART899 significantly reduces tumor growth compared to radiation alone, making it a promising candidate for combination cancer radiotherapy strategies. -
DNA gyrase inhibitor/Hsp90 antagonist
Novobiocin (Albamycin) is a potent and orally active antibiotic that functions as a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. It holds potential for research into highly β-lactam-resistant pneumococcal infections and has demonstrated antiviral activity against orthopoxviruses. -
POLRMT inhibitor
IMT1 is a first-in-class, specific, and noncompetitive inhibitor of human mitochondrial RNA polymerase (POLRMT). It induces a conformational change in POLRMT, preventing substrate binding and inhibiting transcription in a dose-dependent manner in vitro. IMT1 decreases deoxynucleoside triphosphate levels and citric acid cycle intermediates, leading to significant depletion of cellular amino acid levels. IMT1 holds potential for the treatment of diseases associated with mitochondrial transcription disorders. -
WRN inhibitor
HRO761 (Werner syndrome RecQ helicase-IN-1, example 42) is a potent and selective inhibitor of the Werner syndrome RecQ DNA helicase (WRN), an essential enzyme involved in DNA replication, repair, and genome stability. Inhibition of WRN has shown synthetic lethality in cancers with microsatellite instability (MSI) or deficient DNA mismatch repair (dMMR), making HRO761 a promising candidate for targeted cancer therapy. It is being explored in preclinical cancer research to evaluate its efficacy in selectively killing WRN-dependent tumor cells while sparing normal cells. -
PolΘ inhibitor
PolQi2 is a selective inhibitor of DNA polymerase theta (Polθ), specifically targeting its N-terminal helicase domain to suppress the alternative end-joining (alt-EJ) DNA repair pathway. By inhibiting Polθ, PolQi2 enhances the precision and integration efficiency of CRISPR/Cas9-mediated gene editing across diverse genomic loci and cell lines. Furthermore, when used in combination with DNA-PK inhibitors, PolQi2 significantly reduces off-target effects associated with Cas9 activity. These properties make PolQi2 a valuable tool for improving the fidelity and efficiency of gene editing applications in both basic research and potential therapeutic contexts. -
RNA pol III inhibitor
ML-60218 is a broad-spectrum RNA polymerase III (Pol III) inhibitor with IC₅₀ values of 32 μM in *Saccharomyces cerevisiae* and 27 μM in human cells. It inhibits Pol III–mediated transcription, which is essential for the synthesis of small RNAs such as tRNAs and 5S rRNA. ML-60218 has been shown to disrupt pre-assembled viroplasms and prevent the formation of new ones, indicating its antiviral potential. Notably, this activity occurs independently of de novo transcription of host cellular RNAs, suggesting a direct effect on viral replication machinery. ML-60218 is a valuable tool for studying Pol III function and holds potential for antiviral research. -
POLRMT inhibitor
IMT1B (LDC203974) is an orally bioavailable, noncompetitive, and selective allosteric inhibitor of mitochondrial RNA polymerase (POLRMT). By targeting POLRMT, IMT1B disrupts mitochondrial DNA (mtDNA) transcription and impairs mitochondrial gene expression, leading to reduced mitochondrial function. This mechanism contributes to its potent anti-tumor effects, particularly in cancer cells that are highly dependent on mitochondrial metabolism. IMT1B holds promise as a therapeutic agent for targeting mitochondrial vulnerabilities in tumors. -
glutamine amidotransferase inhibitor
Azaserine (CI-337) is a glutamine analog and competitive inhibitor of glutamine amidotransferase, an enzyme involved in nucleotide biosynthesis. It exhibits both antibiotic and antitumor properties by disrupting glutamine-dependent metabolic processes essential for cell proliferation. Azaserine demonstrates antibacterial activity and has shown antitumor effects in various cancer models. However, it has also been reported to possess tumorigenic potential under certain conditions, warranting cautious evaluation. -
POLA1-HDAC11 Inhibitor
GEM144 is a potent and orally bioavailable dual inhibitor of DNA polymerase α (POLA1) and histone deacetylase 11 (HDAC11). It promotes p53 acetylation, induces p21 activation, and triggers G1/S cell cycle arrest followed by apoptosis. GEM144 exhibits significant antitumor efficacy in human orthotopic malignant pleural mesothelioma xenograft models, highlighting its potential as a targeted therapeutic agent for aggressive thoracic malignancies. -
POLA1/HDAC 11 Inhibitor
MIR002 is a potent, orally bioavailable dual inhibitor targeting DNA polymerase α (POLA1) and histone deacetylase 11 (HDAC11). It induces p53 acetylation, upregulates p21 expression, and triggers G1/S cell cycle arrest followed by apoptosis. MIR002 demonstrates significant antitumor efficacy in vivo, highlighting its potential as a therapeutic agent for cancers driven by POLA1 and HDAC11 dysregulation. -
DNA/RNA Synthesis inhibitor
Chlorambucil is a nitrogen mustard alkylating agent.

