BMH-21, a small molecule DNA intercalator, binds ribosomal DNA and inhibits RNA polymerase I (Pol I) transcription and not affects phosphorylation of H2AX.

Quinaldopeptin is a quinomycin antibiotic. It is active against a variety of bacteria, including S. pyogenes, S. aureus, C. perfringens, S. faecalis, E. coli, and K. pneumoniae (MICs = 0.2, 0.4, 0.8, 1.6, 3.1 and 6.3 μg/ml, respectively). It is cytotoxic to B16/F10 and Moser cells (IC50s = 0.0008 and 0.04 μg/ml, respectively) and increases survival in a P388 leukemia mouse model. Quinaldopeptin is a bis-intercalator depsipeptide (NPBID) that binds to and intercalates into DNA (Kd = 32 nM).

Thiocoraline is a depsipeptide and DNAbis-intercalator originally isolated fromMicromonosporawith antibacterial and anticancer activities.1,2It is active against the Gram-positive bacteriaS. aureus,B. subtilis, andM. luteus(MICs = 0.05, 0.05, and 0.03 μg/ml, respectively) but not Gram-negativeE. coli,K. pneumoniae, orP. aeruginosa(MICs = >100 μg/ml for all).1Thiocoraline inhibits RNA and DNA polymerase and thymidylate synthase (IC50s = 6, 6, and 15 μg/ml, respectively), as well as RNA and DNA synthesisin vitro(IC50s = 0.008 and 0.4 μg/ml, respectively). It is cytotoxic to P388, A549, HT-29, and MEL-28 cancer cells (IC50s = 0.002, 0.002, 0.01, and 0.002 μg/ml, respectively). 1.Romero, F., Espilego, F., Pérez Baz, J., et al.Thiocoraline, a new depsipeptide with antitumor activity produced by a marine Micromonospora. I. Taxonomy, fermentation, isolation, and biological activitiesJ. Antibiot. (Tokyo)50(9)734-737(1997) 2.Negri, A., Marco, E., García-Hernández, V., et al.Antitumor activity, X-ray crystal structure, and DNA binding properties of thiocoraline A, a natural bisintercalating thiodepsipeptideJ. Med. Chem.50(14)3322-3333(2007)

Amustaline (S-303) dihydrochloride is a nucleic acid-targeted alkylator recognized for its efficacy as a pathogen inactivation agent in blood components containing red blood cells. This compound comprises three key elements: an acridine anchor (a non-covalently bonding intercalator targeting nucleic acids), an effector (a bis-alkylator group that interacts with nucleophiles), and a linker (a flexible carbon chain with a labile ester bond, hydrolyzing at neutral pH to non-reactive products).

Hycanthone (Etrenol(mesylate)) is a potent drug of antischistosomal. Hycanthone is a DNA intercalator that inhibits RNA synthesis and DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits APE1 via direct protein binding(KD: 10 nM).

AcLysValCit-PABC-DMAE-SW-163D is a drug-linker conjugate for antibody-drug conjugates (ADCs), featuring a natural bis-intercalator, SW-163D, attached through an AcLysValCitPABC-DMAE linker[1].

LMP744 hydrochloride (NSC-706744 hydrochloride) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity. 

Amikhelline is an antimitotic drug. It acts as a DNA intercalator and inhibits DNA polymerase.

Crisnatol, a potent and selective DNA intercalator, has potential anticancer activity.

Pixantrone (BBR 2778 (free base)) hydrochloride is a mitoxantrone analog compound that acts as a topoisomerase II inhibitor and DNA intercalator. It displays anti-tumor activity [1] [2].

Pixantrone has anti-tumor activity that is a DNA intercalator and topoisomerase II inhibitor.

Bisnafide is a Naphthalimide Analogue that acts as DNA intercalator and topo II inhibitor. It is also an antiangiogenic agent. Antiangiogenic agents can normalize tumor vessels and promote the delivery of cytotoxic agents to tumor sites.

BePI can be a specific intercalator of both double and triple-helical DNA.

Crisnatol (BWA770U), an arylmethylaminopropanediol class DNA intercalator, serves as an orally active anticancer agent. It demonstrates in vitro cytotoxicity specifically against human breast cancer cells, while sparing normal human skin fibroblasts.

AQ4 is an inhibitor of topoisomerase II. It is also a DNA intercalator.

LMP744 is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.

Bisnafide is a Naphthalimide Analogue that acts as a DNA intercalator and topo II inhibitor. It is also an antiangiogenic agent that can normalize tumor vessels and promote the delivery of cytotoxic agents to tumor sites.

Bisantrene (CL-216942; NSC 337766) is a topoisomerase II poison and DNA intercalator. It can be used as a Rac1 inhibitor or model compound to study P-glycoprotein-mediated multi-drug resistance (MDR1). Bisantrene inserts and disrupts the configuration of

Pixantrone dimaleate (Pixantrone Maleate) (BBR 2778 dimaleate) is an experimental antineoplastic drug.

BPTQ is a typical intercalator of DNA that acts by inducing a dose-dependent inhibitory effect on the proliferation of cancer cells by arresting cells at the S and G2/M phase.