DNA Damage

Lartesertib is a potent inhibitor of the serine/threonine protein kinase ATM. This compound has demonstrated the ability to inhibit the growth of various hematopoietic cell lines. Furthermore, in combination with the ATR inhibitor Tuvusertib, Lartesertib enhances tumor cell apoptosis and activates immune signaling pathways, showcasing significant anti-tumor efficacy.

(Rac)-Lartesertib is a potent inhibitor of the serine/threonine protein kinase ATM. This compound has demonstrated the ability to inhibit cell proliferation in various hematopoietic cell lines. Moreover, when used in conjunction with the ATR inhibitor Tuvusertib, (Rac)-Lartesertib can enhance tumor cell death, activate immune signaling pathways, and exhibit notable anti-tumor efficacy, making it a valuable tool for cancer research.

MDL-811 is a selective allosteric activator of SIRT6, exhibiting an EC50 of 5.7 μM. This compound demonstrates significant anti-inflammatory, antitumor, and neuroprotective properties, making it a valuable tool for research. MDL-811 is particularly relevant for studies related to colorectal cancer and ischemic stroke, providing insights into potential therapeutic strategies targeting SIRT6 modulation.

Topoisomerase I inhibitor 11 is a potent inhibitor of Topoisomerase I, a key enzyme involved in DNA replication and repair. This compound disrupts the enzyme's catalytic activity, leading to the accumulation of DNA damage and ultimately inducing apoptosis in cancer cells. Topoisomerase I inhibitor 11 is primarily utilized in cancer research, particularly for studying mechanisms of drug resistance and the therapeutic potential of targeting Topoisomerase I in various malignancies.

Anticancer agent 11 functions as a DNA alkylator and crosslinker inducer, exhibiting broad-spectrum anticancer activity. This compound inhibits angiogenesis and promotes the formation of DNA cross-links, leading to disruptions in DNA replication and repair processes. It has potential applications in cancer research, particularly in the study of tumor biology and the development of novel therapeutic strategies.

4-Ketocyclophosphamide is an inactive metabolite that serves as a control for the alkylating agent Cyclophosphamide, functioning as a DNA alkylator and crosslinker. This compound is utilized in research to investigate the mechanisms of action and toxicity of alkylating agents, aiding in the study of cancer therapies and the development of related pharmaceuticals. Its role in understanding the cellular responses to DNA damage makes it valuable for both preclinical and clinical research applications.

Brostallicin is a DNA alkylator and crosslinker known for its potent cytotoxic properties. It effectively induces DNA damage, leading to apoptosis in cancer cells, while exhibiting low myelotoxicity. This compound is primarily utilized in cancer research to explore mechanisms of DNA repair and resistance to therapeutic agents. Its unique profile makes it a valuable tool for advancing studies in oncology and molecular biology.

Canfosfamide hydrochloride functions as a DNA alkylator and crosslinker. Upon activation by the enzyme glutathione S-transferase P1-1 (GSTP1-1), it generates an active anticancer alkylating agent alongside a glutathione derivative. This compound is primarily utilized in cancer research to investigate its therapeutic potential and mechanisms of action in tumor cell lines.

A-966492 displayed high potency against the poly(ADP-ribose) polymerase-1 (PARP-1) enzyme with a K(i) of 1 nM and an EC(50) of 1 nM in a whole cell assay.

ABT-492 is a new fluoroquinolone against 155 aerobic and 171 anaerobic pathogens.

Alendronate is a nitrogen-containing bisphosphonate that is commonly used in the treatment of osteoporosis and other metabolic bone diseases.

Altretamine is classified as an alkylating antineoplastic agent.This unique structure is believed to damage tumor cells through the production of the weakly alkylating species formaldehyde, a product of CYP450-mediated N-demethylation.

Bendamustine Hydrochloride is a small molecule bifunctional DNA alkylating agent, combining a nitrogen mustard functionality with a purine-analog structure. The dense DNA-damaging functionality of Bendamustine differentiates it from other compounds used as antiproliferative agents, and these functionalities are thought to promote cell death through a variety of different pathways including apoptosis and mitotic catastrophe.

Cerubidine (Daunorubicin HCl, Rubidomycin HCl) interacts with DNA by intercalation and inhibition of macromolecular biosynthesis. This inhibits the progression of the enzyme topoisomerase II, which relaxes supercoils in DNA for transcription. It stabilizes the topoisomerase II complex after it has broken the DNA chain for replication, preventing the DNA double helix from being resealed and thereby stopping the process of replication.

Costunolide is an Inhibitor of human telomerase activity (IC50 = 65 μM in MCF-7 breast cancer cells). It is described to act as an antioxidant, anti-mycobacterial, anti-inflammatory, and anti-viral, with cytotoxic activity.

CUDC-101 is a novel compound which inhibits multiple targets, which is designed to inhibit HDAC, EGFR and Her2.

Dacarbazine is an antineoplastic chemotherapy drug used in the treatment of various cancers.Dacarbazine is a member of the class of alkylating agents, which destroy cancer cells by adding an alkyl group (CnH2n+1) to its DNA.

Droxinostat is a selective inhibitor of HDAC3, HDAC6, and HDAC8 that shows comparable inhibition of HDAC6 and HDAC8 with IC50 = 2.47 and 1.46 μmol/L, respectively.

Epirubicin is a cell-permeable anthracycline antitumor antibiotic. It is a stereoisomer(4?€?-epi-isomer) of doxorubicin that exhibits reduced cardiotoxicity. It is used to inhibit topoisomerase II and DNA helicase activity.

Floxuridine is an oncology drug that belongs to the class known as antimetabolites.

Fludarabine or fludarabine phosphate (Fludara) is a chemotherapy drug used in the treatment of hematological malignancies (cancers of blood cells such as leukemias and lymphomas) .Fludarabine inhibits DNA synthesis by interfering with ribonucleotide reductase and DNA polymerase. It is active against both dividing and resting cells.

Gatifloxacin is a fluoroquinolone antibiotic which inhibits bacterial DNA gyrase (IC50 = 0.109 ng/ml) and topoisomerase IV (IC50 = 13.8 ng/ml).

Ifosfamide is a cytostatic agent that is structurally related to cyclophosphamide.

Levofloxacin is a fluoroquinolone antibiotic. It is active against S. aureus, S. epidermidis, B. subtilis, E. coli, P. aeruginosa, and K. pneumoniae (MICs = 0.25, 0.25, 0.5, 0.03, 4, and 0.25 μg/ml, respectively).

Lincomycin is a lincosamide antibiotic isolated from Streptomyces lincolnensis which is reported to inhibit bacterial protein synthesis and is concentration dependent.

Lomustine is an alkylating nitrosourea compound that possesses antitumor activity similar to Carmustine causing DNA interstrand cross-linking.

Marbofloxacin is a potent antibiotic of the 3rd generation fluoroquinolone group and acts by inhibiting bacterial DNA replication.

Mercaptopurine has been shown to interfere with DNA and RNA synthesis and cause inhibition of de novo purine syntehsis.

Mitoxantrone is a synthetic antineoplastic anthracenedione (IC50 = 0.42 mM).

Mitoxantrone Dihydrochloride is an antiviral, antibacterial, antiprotozoal, immunomodulating, and antineoplastic cytostatic anthraquinone derivative.

Mizoribine is an imidazole nucleoside immunosuppressant agent that was first isolated from the mold Eupenicillium brefeldimium with antibiotic and cytotoxic effects.

Nelarabine is a purine nucleoside analog converted to its corresponding arabinosylguanine nucleotide triphosphate (araGTP), resulting in inhibition of DNA synthesis and cytotoxicity.

Norfloxacin(Norxacin) is a broad-spectrum antibiotic.

Ofloxacin is a synthetic broad-spectrum antimicrobial agent.

Parthenolide ((-)-Parthenolide) is a sesquiterpene lactone which occurs naturally in the plant feverfew (Tanacetum parthenium).

Podophyllotoxin is a potent inhibitor of microtubule assembly that binds at the colchicine site of tubulin.

Pyroxamide (NSC 696085) is a potent inhibitor of affinity-purified HDAC1 and causes the accumulation of acetylated core histones in MEL cells cultured with the agent.

Sodium butyrate (NaB, Butanoic acid sodium salt), sodium salt of butyric acid, is a histone deacetylase inhibitor and competitively binds to the zinc sites of class I and II histone deacetylases (HDACs).

Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2.

Teniposide is a semisynthetic derivative of podophyllotoxin with antineoplastic activity.

Tenofovir is in a class of medications called nucleoside reverse transcriptase inhibitors (NRTIs). It works by decreasing the amount of HIV in the blood.

Thiotepa is a polyfunctional, organophosphorus alkylating agent and a stable derivative of N,N',N''-triethylenephosphoramide (TEPA), with antineoplastic activity.

Topotecan HCl (Hycamtin) is a chemotherapeutic agent that is a topoisomerase inhibitor.

Trifluridine is an anti-herpesvirus antiviral drug, used primarily on the eye. It was sold under the trade name, Viroptic, by Glaxo Wellcome, now merged into GlaxoSmithKline.

Tubacin (tubulin acetylation inducer) is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM.

Zalcitabine is a potent nucleoside analogue reverse transcriptase inhibitor used in the treatment of HIV infection.

CP-466722 is a specific ATM inhibitor that inhibits cellular ATM-dependent phosphorylation events and disruption of ATM function resulted in characteristic cell cycle checkpoint defects.

Pneumocandin B0 is the major analogue of a family of lipopeptides isolated from several species of several different genera, notably Cryptosporiopsis, Glarea and Pezicula. Pneumocandin B0 is a potent antifungal and acts by inhibition of the synthesis of β-(1,3)-D-glucan, an essential component of the cell wall of susceptible fungi.

Abacavir is a nucleoside analog reverse transcriptase inhibitor (NRTI); guanosine analog used to treat HIV and AIDS.