DNA Damage

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-888(Veliparib) is a potential anti-cancer drug acting as a PARP 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.

Adriamycin is an anthracycline antibiotic, it works by intercalating DNA, while most serious adverse effect being life-threatening heart damage. It is commonly used in the treatment of a wide range of cancers, including hematological malignancies, many types of carcinoma, and soft tissue sarcomas.

Fluorouracil (Adrucil) is a suicide inhibitor and works through irreversible inhibition of thymidylate synthase.

AG-014699 (Rucaparib) is a PARP inhibitor that inhibits poly(ADP-ribose) polymerase (PARP) is a key enzyme in DNA repair.

AG14361 is a potent PARP inhibitor, enhanced TMZ cytotoxicity in MMR(mismatch repair)-proficient / deficient cells.

Amonafide is a DNA intercalator and topoisomerase II inhibitor for the treatment of neoplastic diseases, one of Antitumor agent.

Olaparib (AZD2281) is an inhibitor of poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair.

Belinostat (PXD101) is a HDAC inhibitor that inhibits HDAC activity in HeLa cell extracts with an IC50 of 27 nM.

BEZ235 (NVP-BEZ235) inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes.

BIBR 1532 is a selective telomerase inhibitor (IC50 values are 93, > 100000 and > 100000 nM for human telomerase, human RNA polymerase I and human RNA polymerase II + III respectively).

Bleomycin sulfate is a mixture of the sulfate salts of basic glycopeptide antineoplastic antibiotics isolated from Streptomyces verticillus.

BSI-201 is a potent inhibitor of PARP-1 and has been shown to cross the blood-brain barrier.

Camptothecin is a cytotoxic quinoline alkaloid which inhibits the DNA enzyme topoisomerase I (topo I).

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.

Cidofovir (Vistide) is an antiviral used for the treatment of cytomegalovirus (CMV) infection (ie: retinitis).

Clofarabine is a second generation purine nucleoside analog with antineoplastic activity

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.

Daptomycin is a lipopeptide antibiotic used in the treatment of certain infections caused by Gram-positive organisms.

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.

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.

Etoposide forms a ternary complex with DNA and the topoisomerase II enzyme (which aids in DNA unwinding), prevents re-ligation of the DNA strands, and by doing so causes DNA strands to break. Therefore, this causes errors in DNA synthesis and promotes apoptosis of the cancer cell.

EX 527 is a potent and selective SIRT1 class III histone deacetylase enzyme inhibitor with IC50 of 38 nM in a cell-free assay.

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

Tegafur is a chemotherapeutic 5-FU prodrug used in the treatment of cancers. It is a component of tegafur-uracil.

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

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.

Idarubicin is an anthracycline antibiotic that is an anti-leukemia agent with higher DNA binding capacity and greater cytotoxicity than daunorubicin.

3-Aminobenzamide is a novel PARP inhibitor, known to sensitize cells to radiation in vitro by inhibiting the repair of DNA damage.

Irinotecan prevents DNA from unwinding by inhibition of topoisomerase 1.

Irinotecan (CPT 11), a compound within the camptothecin family, is an inhibitor of topoisomerase 1 involved in cellular DNA replication and transcription.

ITF2357 (Givinostat) is a HDACs inhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities.

JNJ-26481585 (Quisinostat) is a pan-HDAC inhibitor with marked potency toward HDAC1 (IC(50), 0.16 nmol/L).

KU-55933 is an ATM inhibitor by suppressing cell proliferation and induces apoptosis by blocking Akt in cancer cells with overactivated Akt.

KU-60019 is a potent and specific ATM inhibitor with IC50 of 6.3 nM.

LAQ824 (NVP-LAQ824) is a potent novel histone deacetylase inhibitor with significant activity against multiple myeloma.

LBH589 is a hydroxamic acid and acts as a non-selective HDAC inhibitor with IC5o of HDAC1 to be 0.23 nM.

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

MC1568 is a member of HDAC inhibitors that inhibits the histone deacetylase class II by modifying the genetic expression of various important genes of cell cycle mostly at G1 phase, resulting in the death of breast cancer cells by apoptosis.

MGCD0103 (Mocetinostat) is a benzamide histone deacetylase inhibitor by inhibiting mainly histone deacetylase 1 (HDAC1), but also HDAC2, HDAC3, and HDAC11.

Moxifloxacin is a quinolone/fluoroquinolone antibiotic.

MS-275 (Entinostat) is a potent HDAC inhibitor with IC50 of 0.3 and 8uM for HDAC1 and HDAC3, respectively.

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).

PCI-24781 is a broad-spectrum phenyl hydroxamic acid HDAC inhibitor.

PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of phosphatidylinositol 3-kinase (PI3K) family members with selectivity toward DNA-PK, PI3K (p110α), and mTOR.