Bleomycin sulfate (Blenoxane) is a glycopeptide antibiotic and an anticancer agent for squamous cell carcinomas (SCC) with IC50 of 4 nM in UT-SCC-19A cells.

BMH-21 is a small molecule DNA intercalator that binds ribosomal DNA and inhibits RNA polymerase I transcription; does not cause phosphorylation of H2AX.

COH29 is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity with an IC50 of 8 μM in KB cell.

CX-5461 is an inhibitor of rRNA synthesis, selectively inhibits Pol I-driven transcription of rRNA, has no effect on Pol II, and possesses 250-to 300-fold selectivity for inhibition of rRNA transcription versus DNA replication and protein translation.

Dactinomycin (also known generically as Actinomycin D ) is the most significant member of actinomycines, which are a class of polypeptide antibiotics isolated from soil bacteria of the genus Streptomyces.

Quarfloxin (CX-3543) is a fluoroquinolone derivative with antineoplastic activity.

TH 287 is a first-in-class MTH1 inhibitor (IC50 value 5.0 nM) that selectively and effectively kills U2OS and other cancer cell lines, with considerably less toxicity towards several primary or immortalized cells.

TH588 is a novel potent, selective and cell permeable inhibitor of the nudix hydrolase family MTH1 protein with an IC50 of ~5 nM.

Rifalazil (KRM-1648; ABI-1648), a rifamycin derivative, inhibits the bacterial DNA-dependent RNA polymerase and kills bacterial cells by blocking off the β-subunit in RNA polymerase. Rifalazil (KRM-1648; ABI-1648) is an antibiotic, exhibits high potency against mycobacteria, gram-positive bacteria, Helicobacter pylori, C. pneumoniae and C. trachomatis with MIC values from 0.00025 to 0.0025 μg/ml. Rifalazil (KRM-1648; ABI-1648) has the potential for the treatment of Chlamydia infection, Clostridium difficile associated diarrhea (CDAD), and tuberculosis (TB).

Caracemide (NSC-253272) inhibits the enzyme ribonucleotide reductase of Escherichia coli. Caracemide is a novel anticancer agent derived from a hydroxamic acid and has demonstrated to produce severe central nervous system (CNS) toxicity.

Sorivudine (BV-araU) is an orally active synthetic pyrimidine nucleoside antimetabolite drug. Sorivudine derives its antiviral activity from selective conversion by a specific thymidine kinase present in certain DNA viruses to nucleotides, which can in turn interfere with viral DNA synthesis.

T-705RTP sodium, a nucleotide analog, selectively inhibits RNA-dependent RNA polymerase (RdRp) of the influenza virus. T-705RTP sodium competitively incorporates ATP/GTP and a single molecule of T-705RTP sodium is incorporated into a nascent RNA strand, which then inhibits subsequent virus RNA extension.

T-705RTP is a selective and GTP-competitive influenza virus RNA polymerase inhibitor with an IC50 of 0.14 μM and a Ki of 1.52 μM. T-705RTP is the active triphosphate metabolite of T-705 and has potent anti-influenza virus activity.

BCH001 is a specific PAPD5 inhibitor that restores telomerase activity and telomere length in dyskeratosis congenita (DC) patient induced pluripotent stem cells. PAPD5 is a noncanonical poly(A) polymerase with an unusual RNA-binding motif.

JH-RE-06 is a potent REV1-REV7 interface inhibitor with an IC50 of 0.78 μM and Kd value of 0.42 μM, disrupting REV1-POL ζ-mediated mutagenic translesion synthesis (TLS).

Mafosfamide sodium salt (Z 7557 sodium salt) targets nuclear DNA, forms DNA cross-links and inhibits DNA synthesis. Mafosfamide sodium salt, a cyclophosphamide analogue, induces apoptosis in lymphoblastoid cells. Mafosfamide sodium salt has antitumor activity.

Tezacitabine is a cytostatic and cytotoxic antimetabolite and a nucleoside analogue. Tezacitabine irreversibly inhibits the ribonucleotide reductase and interferes with DNA replication and repair. Tezacitabine effectively induces cells apoptotic. Tezacitabine has the potential for leukemias and solid tumors (carcinomas) treatment.

Riddelline, a pyrrolizidine alkaloid, is a potent genotoxic agent. Riddelline induces significant elevations in unscheduled DNA synthesis and S-phase synthesis in rat liver.

GS-443902 (GS-441524 triphosphate) is a potent viral RNA-dependent RNA-polymerases (RdRp) inhibitor with IC50s of 1.1 μM, 5 μM for RSV RdRp and HCV RdRp, respectively. GS-443902 is the active triphosphate metabolite of Remdesivir.

γ-Amanitin an ADC cytotoxin and isolated from the?mushroom. γ-Amanitin inhibits?RNA polymerase II and disrupts synthesis of?mRNA. γ-Amanitin shows similar effects to α-Amanitin and β-Amanitin .

ε-Amanitin, a cyclic peptide isolated from a variety of mushroom species, potently binds to and inhibits the activity of RNA polymerase II.

Bromochloroacetonitrile is a by-product of the chlorine disinfection of water containing natural organic material. Bromochloroacetonitrile possesses direct acting mutagenic activity and is capable of inducing DNA strand breakage.