cross-linking

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.

Rimiducid is a lipid-permeable tacrolimus analogue, homodimerizing an analogue of human protein fkbp12 and binding to wild-type fkbp12 with 1000-fold lower affinity. Rimiducid is a dimerizer agent that acts by cross-linking the FKBP domains. It dimerizes the Caspase 9 suicide switch and rapidly induces apoptosis.

Cisplatin (CDDP) is a DNA cross-linking agent. Cisplatin has antitumor activity and inhibits DNA synthesis by forming DNA adducts in cancer cells. Cisplatin also activates ferroptosis and induces autophagy.

Cefuroxime Sodium is the sodium salt form of cefuroxime and a semi-synthetic, broad-spectrum, beta-lactamase resistant, second-generation cephalosporin antibiotic with bactericidal activity. Cefuroxime sodium (Cefuroxime sodium salt) inhibits bacterial cell wall synthesis by inactivating penicillin binding proteins (PBPs) thereby interfering with the final transpeptidation step required for cross-linking of peptidoglycan units which are a component of the cell wall. Lack of cross-linking results in a reduction of cell wall stability and leads to cell lysis.

Biotin-LC-LC-NHS, an SMCC cross-linking reagent, acts as a labeling agent for antibodies and small molecules (like Paclitaxel).

PXS-6302 is an irreversible inhibitor of lysyl oxidase with IC50s of 3.7 μM for Bovine LOX, 3.4 μM for rh LOXL1, 0.4 μM for rh LOXL2, 1.5 μM for rh LOXL3, 0.3 μM for rh LOXL4, respectively. PXS-6302 can readily penetrate the skin, reduces collagen deposition and cross-linking, and significantly improves scar appearance without reducing tissue strength. PXS-6302 also has potentially broader applications in other fibrotic diseases.

Bendamustine D4 is the deuterium-labeled Bendamustine. Bendamustine is a DNA cross-linking compound with alkylating and antimetabolite properties. Bendamustine causes DNA breaks.

Modotuximab (Anti-Human EGFR Recombinant Antibody), an IgG1κ-type chimeric antibody, selectively binds to human EGFR protein. Incorporating elements from Futuximab, it targets two distinct, non-overlapping epitopes on EGFR, facilitating receptor cross-linking, subsequent cellular internalization, and degradation, thereby conferring its antitumor activity in vivo [1].

WEHI-150 is an analog of mitoxantrone, a DNA interstrand cross-linker (t1/2=12.5 h). WEHI-150 is capable of forming covalent adducts on CpG sequences, with a particular preference for methylated CpG sites. Formaldehyde-activated WEHI-150 induces DNA interstrand cross-linking and blocks transcription in a concentration-dependent manner. WEHI-150 mediates the formation of covalent adducts that do not interact with guanine N-2 and forms adducts on new DNA sequences.

Sulfo-SMPB sodium is a non-cleavable, heterobifunctional chemical cross-linking reagent that combines N-hydroxysuccinimide ester and maleimide groups, enabling the covalent conjugation of molecules possessing (amine) and (sulfhydryl) functionalities.

Isodityrosine is a new cross-linking amino acid from plant cell-wall glycoprotein.

2-(Pyridyldithio)ethylamine hydrochloride ((S)-2-Pyridylthio Cysteamine Hydrochloride) is a disulfide intercalating cross-linking reagent.

PR-104 sodium is a hypoxia-activated DNA cross-linking agent used in the research of tumor xenograft models. It functions as a nitrogen mustard pre-prodrug and efficiently transforms into the more lipophilic dinitrobenzamide mustards alcohol PR-104A.

4-Oxo-2-nonanal (4-ONE) is a lipid peroxidation product that actively modifies histidine and lysine residues in proteins, leading to protein cross-linking, and alters 2'-deoxyguanosine, indicating its role in mutagenesis and carcinogenesis. 4-ONE alkyne, an alkyne-tagged electrophile, serves as a probe for isolating and identifying lipid peroxidation reaction products through click chemistry.

Glyfosfin is a DNA cross-linking agent and an alkylating agent with anticancer activity.

N,N'-Carbonyldiimidazole is a biological cross-linking agent that has great application in mass spectrometry to detect the purity of compounds.

Dityrosine, an oxidation product of protein formed through the intermolecular cross-linking of tyrosyl radicals from the reactive oxygen species (ROS) and tyrosine interaction, is associated with decreased hippocampal expression of NMDA receptor subunits Nr1, Nr2a, and Nr2b when administered intragastrically at 320 µg/kg per day, leading to memory impairments in mice as evidenced by their performance in a novel object recognition test. Additionally, it raises fasting blood glucose levels while reducing plasma insulin levels and the pancreatic expression of insulin synthesis-related genes Ins2, Pdx1, and MafA. Increased dityrosine levels have been positively linked to a range of diseases, including autism spectrum disorder, cataracts, Alzheimer’s disease, Parkinson’s disease, atherosclerosis, and cystic fibrosis.

Transglutaminase (TG) is a thiolase that induces intermolecular cross-linking of proteins, by catalysing the formation of isopeptide bonds between the γ-carboxamide group of glutamine residues and the primary ε-amine group of other compounds. The enzyme plays a role in a variety of physiological processes including coagulation, antimicrobial immune responses and photosynthesis.

DSSeb Crosslinker is a homobifunctional cross-linking reagent. It is useful in protein crosslinking and making antibody-drug conjugates.

Yoshi-864 alkylates and cross-links DNA, thereby inhibiting DNA replication. It is an alkyl sulfonate DNA cross-linking agent with potential anti-cancer activity.

Bizelesin is a synthetic cyclopropylpyrroloindole antineoplastic antibiotic. Bizelesin binds to the minor groove of DNA and induces interstrand cross-linking of DNA, thereby inhibiting DNA replication and RNA synthesis. Bizelesin also enhances p53 and p21 induction and triggers G2/M cell-cycle arrest, resulting in cell senescence without apoptosis.

UBE2T FANCL-IN-1 is a potent inhibitor of UBE2T FANCL-mediated FANCD2 monoubiquitylation, significantly enhancing cellular sensitivity to Carboplatin, a DNA cross-linking agent.

Jacobine induces significant dose-dependent DNA-DNA interstrand cross-linking over the entire range of doses. It was catalyzed by guinea pig hepatic glutathione-S-transferase enzymes in in vitro experiments.

Bostrycin, an anthraquinone derived from B. alpestre, exhibits a broad spectrum of biological activities including antibacterial, antiproliferative, and phytotoxic effects. This compound demonstrates efficacy against Gram-positive bacteria like methicillin-resistant S. aureus (MRSA), M. tuberculosis, and C. botulinum. Additionally, Bostrycin shows antiproliferative action against A549 lung adenocarcinoma cells, particularly by arresting the cell cycle at the G0/G1 phase and triggering apoptosis within a concentration range of 10 to 30 µM. As a phytotoxin, it causes necrosis in water hyacinth leaves at approximately 7 µg/ml. Furthermore, Bostrycin serves as a protein immobilization cross-linking agent, managing to preserve its bacteriostatic properties when affixed to nonwoven polypropylene fabric.

Ceforanide is a second-generation cephalosporin antibiotic with bactericidal activity. Ceforanide causes inhibition of bacterial cell wall synthesis by inactivating penicillin binding proteins (PBPs) thereby interfering with the final transpeptidation ste

Chlorpyrifos-oxon, an active metabolite of Chlorpyrifos, is a potent phosphorylating agent that significantly inhibits AChE activity and induces cross-linking between tubulin subunits, thereby disrupting microtubule function [4].

Cefdinir monohydrate is the salt form of Cefdinir (free base), a semi-synthetic cephalosporin and a beta-lactam antibiotic with bactericidal activity. Cefdinir's effect is dependent on its binding to penicillin-binding proteins (PBPs) located in the bacterial cytoplasmic membrane. Binding results in the inhibition of the transpeptidase enzymes, thereby preventing cross-linking of the pentaglycine bridge with the fourth residue of the pentapeptide and interrupting consequent synthesis of peptidoglycan chains. As a result, cefdinir inhibits bacterial septum and cell wall synthesis formation.

SJG-136, a DNA cross-linking agent (XL50: 45 nM for pBR322 DNA), is used for its capability to form covalent bonds between DNA strands.

4-hydroxy Nonenal is a lipid peroxidation product derived from oxidized ω-6 polyunsaturated fatty acids such as arachidonic acid and linoleic acid. [1] [2] It exhibits various biological activities such as cytotoxicity, growth inhibiting activity, genotoxicity, and chemotactic activity and has been widely used as a marker of lipid peroxidation.[1][2][3] 4-oxo-2-Nonenal is a more recently identified product of lipid peroxidation.[4][5][6] It actively modifies histidine and lysine residues on proteins and causes protein cross-linking. [7][8] 4-oxo-2-Nonenal also modifies 2’-deoxyguanosine, further implicating lipid peroxidation in mutagenesis and carcinogenesis.[4]

Englumafusp alfa (CD19-4-1BBL; RO7227166) is a fusion protein that combines a CD19-specific antibody domain with trimerized extracellular domains of human 4-1BBL, engineered to induce CD19-specific 4-1BB cross-linking on T and NK cell surfaces [1].