damaging

Auristatin F is an effective inhibitor of microtubule and vascular damaging agent. Auristatin F can be used in antibody-drug conjugates.

Trimethylamine N-oxide (TMAO) is a gut microbiota-dependent metabolite derived from dietary choline, betaine, and carnitine. It induces inflammation by activating the ROS/NLRP3 inflammasome and promotes fibroblast differentiation through the activation of the TGF-β/Smad2 signaling pathway. TMAO is commonly used to induce cardiac fibrosis models.

Bleomycin sulfate is a glycopeptide antibiotic with antitumor activity. It is commonly used as a DNA-damaging agent and DNA synthesis inhibitor. It functions by inducing DNA strand breaks without affecting RNA strands. Bleomycin sulfate is widely used in cancer research and for establishing pulmonary fibrosis animal models.

Bleomycin hydrochloride is a glycopeptide antibiotic and a DNA synthesis inhibitor. Bleomycin Sulfate can cause DNA strand breaks but not RNA strand breaks. Bleomycin Sulfate has anti-tumor activity.

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.

Pyridinium bisretinoid A2E (A2E) is a fluorescent chromophore isolated from lipofuscin in retinal pigment epithelium, a lipophilic cation and weak photosensitizer with cytotoxicity. A2E promotes apoptosis under blue light exposure and induces autophagy under photoactivation, damaging membrane integrity in a concentration-dependent manner.

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.

ZNL 02-096 (Pomalidomide-C3-adavosertib) is a rapid and selective degrader of Wee1 (IC50=3.58 nM).ZNL 02-096 selectively degrades Wee1 at submolar concentrations without damaging PLK1, a secondary target of AZD 1775.ZNL 02-096 induces degradation of Wee1 and accumulation of DNA damage in MOLT-4 cells in vitro, In vitro in MOLT-4 cells, ZNL 02-096 induced Wee1 degradation, accumulation of DNA damage, cell cycle arrest in G2/M phase and apoptosis.ZNL 02-096 showed anti-proliferative effects in 300 cancer cell lines.

Tioconazole (Vagistat) is a synthetic imidazole derivative, inhibits cell wall synthesis by inhibiting the biosynthesis of ergosterol or other sterols, damaging the fungal cell membrane, altering its permeability, and promoting loss of essential intracellular elements.

Terconazole (Terazol 7) is a synthetic triazole derivative structurally related to fluconazole, antifungal Terconazole seems to disrupt cell wall synthesis by inhibiting biosynthesis of ergosterol or other sterols, damaging the fungal cell membrane, altering its permeability, and promoting loss of essential intracellular elements. Terconazole is active against Candida sp.

Fenobucarb is a broad-spectrum carbamate insecticide and AChE inhibitor primarily used to control various flukes damaging crops. It exhibits neurotoxicity to zebrafish foetal development and induces muscle spasms and paralysis in insects, fish, and mammals.

Alloxan Monohydrate is a diabetogenic agent that acts as a proteasome inhibitor and induces diabetes in experimental animals by damaging the insulin-secreting β-cells in the pancreas. It is commonly used to establish diabetes models.

Neocarzinostatin is an effective DNA-damaging, anti-tumor antibiotic. It recognizes double-stranded DNA bulge and induces DNA double strand breaks (DSBs). Neocarzinostatin leads to apoptosis. Neocarzinostatin has potential for EpCAM-positive cancer treatment.

Compound 23, known as Top1/2-IN-1, is a dual inhibitor of Top1/2 that can be administered orally and exhibits antiproliferative effects. It induces apoptosis and cell cycle arrest in cancer cells by damaging DNA and elevating reactive oxygen species levels. Additionally, Top1/2-IN-1 demonstrates antitumor activity in vivo within xenograft models.

MG28 exhibits significant cytotoxic effects, likely stemming from its direct and potent DNA-damaging activity. The compound is utilized in cancer research.

N-Ethyl-N-nitrosourea (ENU) is a DNA alkylating agent. It induces leukemia by alkylating nucleobases, thereby damaging DNA, which leads to bone marrow suppression and the development of leukemia cells. ENU is teratogenic in vivo, causing tumor formation and foot malformations in pregnant rats. Additionally, it can result in central nervous system (CNS) tumors and genetic disorders.

Empenthrin, a synthetic pyrethroid used in insecticides, is active against broad spectrum of flying insects including moths and other pests damaging textile.

CHK1-IN-9 (compound 11) is an orally active CHK1 inhibitor with an IC50 of 0.55 nM. It enhances the effects of DNA-damaging agents on tumor cells and exhibits synergistic anticancer activity with Gemcitabine.

ERCC1/XPA interaction inhibitor 1 (compound 27o) is a potent inhibitor of the ERCC1/XPA67-80 interaction, with an EC50 value of 4.7 µM. This compound shows potential for studying DNA-damaging agents and overcoming resistance to platinum-based chemotherapy.

KDX1381 is a bivalent CK2α inhibitor with an IC50 of 17 nM and a KD of 54 nM. It demonstrates antitumor activity in murine 786-O and A375 xenograft models. Furthermore, when combined with a vascular endothelial growth factor receptor (VEGFR) inhibitor or DNA-damaging agents, KDX1381 enhances antitumor effects in mouse hepatocellular carcinoma and glioma models.

L-Ascorbic acid (L-Ascorbate) magnesium is an electron donor and an endogenous antioxidant. It selectively inhibits Cav3.2 channels with an IC50 of 6.5 μM. Additionally, L-Ascorbic acid promotes collagen deposition and inhibits elastin production. It also exhibits anticancer effects by generating reactive oxygen species (ROS) and selectively damaging cancer cells.

HLI373 is an efficacious Hdm2 inhibitor, an ubiquitin ligase (E3), effective in inducing apoptosis of several tumor cells sensitive to DNA-damaging agents [1], and also shows prominent antimalarial activity [2].

Irofulven is an agent of DNA-damaging and antitumor. It is used for the treatment of advanced solid tumors, including prostate, ovarian, and pancreatic cancers.

(S,S)-D211 is a DNA damaging payload.