DNA-damage

Amifostine (Ethyol) anhydrous is a cytoprotective agent, acts as a free radical scavenging activity.

Amifostine trihydrate (WR2721) is the first approved radioprotective drug, used to decrease the risk of kidney problems caused by treatment with cisplatin.

Ciprofloxacin monohydrochloride (Bay-09867 hydrochloride) is a broad-spectrum antimicrobial carboxyfluoroquinoline.

Avermectin B1 is served as anthelmintic and insecticide.

Ciprofloxacin (Bay-09867) mainly targets bacterial DNA Gyrase (IC50=0.22-0.31 µM) and topoisomerase IV (IC50=0.3-1.9 µM). Ciprofloxacin is a highly active fluoroquinolone antibiotic.

Ciprofloxacin hydrochloride monohydrate (Bay-09867 hydrochloride monohydrate) is a fluoroquinolone antibiotic,is an antibiotic used to treat a number of bacterial infections

Phleomycin is one of the anticancer glycopeptide antibiotics which cause DNA cleavage. It is similar to Bleomycin which binds and intercalates DNA to damage the integrity of the double helix.

Cjoc42 is an inhibitor of gankyrin, an ankyrin-repeat oncoprotein whose overexpression has been implicated in the development of many cancer types. cjoc42 prevents the decrease in p53 protein levels normally associated with high amounts of gankyrin, and it restores p53-dependent transcription and sensitivity to DNA damage

L67 (DNA Ligase Inhibitor) is a competitive inhibitor of human DNA ligases I and III with an IC50 of 10 μM.

Mollugin (Rubimaillin) may be a JAK2 inhibitor and inhibits LPS-induced inflammatory responses by blocking the activation of the JAK-STAT pathway. Mollugin as a candidate for a chemotherapeutic agent in OSCCs via the upregulation of the HO-1 and Nrf2 pathways and the downregulation of NF- κ B. Mollugin may be a novel therapeutic candidate for bone loss-associated disorders including osteoporosis, rheumatoid arthritis, and periodontitis. Also, it has anticancer efficacy, can modulate the HER2 pathway in HER2-overexpressing Y cells with a potential role in the treatment and prevention of human breast and ovarian Y with HER2 overexpression.

KPT-6566 is a novel selective covalent pin1 inhibitor, KPT-6566 shows an IC50 of 640 nM and a Ki of 625.2 nM for PIN1 PPIase domain,and has anti-cancer activity.

CCT128930 hydrochloride (CCT128930 hydrochloride) is a potent and selective inhibitor of AKT with IC50 of 6 nM. CCT128930 hydrochloride induces cell cycle arrest, DNA damage, and autophagy. CCT128930 hydrochloride has 28-fold selectivity over the closely related PKA kinase (IC50: 168 nM) through the targeting of Met282 of AKT, as well as 20-fold selectivity over p70S6K (IC50: 120 nM).

B355252 protects against cell death caused by glutamate-evoked oxidative stress. B355252 shows neuroprotective effect, potentiating nerve growth factor (NGF)-induced neurite outgrowth.

Bractoppin is a drug-like inhibitor of phosphopeptide recognition by the human BRCA1 tandem (t)BRCT domain (IC50 = 0.074 μM), which selectively inhibits substrate binding with nanomolar potency in vitro. Structure-activity exploration suggests that Bractoppin engages BRCA1 tBRCT residues recognizing pSer in the consensus motif, pSer-Pro-Thr-Phe, plus an abutting hydrophobic pocket that is distinct in structurally related BRCT domains, conferring selectivity.

Rad51-in-1 is a derivative of B02 and an effective inhibitor of Rad51.

HQ461 is a molecular glue that promotes CDK12-DDB1 interaction, triggering cyclin K degradation, decreased CDK12 substrate phosphorylation, downregulation of DNA damage response genes, and cell death.

Oxaliplatin (L-OHP) is a DNA alkylating agent, an inhibitor of DNA synthesis. Oxaliplatin causes DNA cross-linking damage, preventing DNA replication and transcription and leading to cell death. Oxaliplatin induces autophagy.

(-)-Epigallocatechin Gallate (EGCG) is a phenolic antioxidant polyphenol flavonoid found in plants such as green and black tea, which inhibits telomerase and DNA methyltransferase, blocks the activation of EGF receptors and HER-2 receptors, inhibits cellular oxidation, and prevents free radical damage to cells.

Trastuzumab is a humanized monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab has been clinically used to treat HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer.

Cisplatin (CDDP) is a chemotherapeutic agent with antitumor activity and is a classic DNA crosslinker. It inhibits DNA synthesis and induces DNA damage in cancer cells by forming DNA adducts, ultimately leading to cell death. In addition, Cisplatin can activate ferroptosis and induce autophagy. In animal studies, it is commonly used to establish models of chronic kidney injury and acute renal failure.

Talazoparib (LT-673) is a new-type PARP inhibitor (IC50: 0.58 nM), It similarly binds to PARP1/2 (Kis: 1.2/0.85 nM).

Elimusertib (BAY-1895344) is a potent, highly selective, and orally available ATR inhibitor with an IC50 of 7 nM, demonstrating significant anti-tumor efficacy as a monotherapy and strong combination potential with targeted alpha therapy Radium-223 dichloride.

Azoxymethane (AOM) is a colon-specific carcinogen that induces DNA damage and forms DNA adducts, and is commonly used to establish mouse models of colorectal cancer.

AOH1996 is an orally active ligand for the replicasome component PCNA (proliferating cell nuclear antigen), targeting the transcription-replication conflict (TRC). It interferes with the interaction of PCNA with its binding proteins, leading to DNA replication stress and apoptosis. AOH1996 causes proteasome-dependent rpb1 degradation and lethal DNA damage by stabilizing the interaction between PCNA and RNA polymerase II, and acts synergistically with DNA damaging agents to inhibit tumor cell growth.