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Diazirine linkers, such as trifluoromethyl phenyl DAs and alkyl DAs, generate reactive carbene species via loss of N2 upon photoirradiation at 350 nm employing photo induced cross linking. This active carbene easily inserts into neighboring C–H or heteroatom–H bonds and forms a covalent adduct by a photoreactive linker. Additionally, the generated carbene has a quick half-life in the nanosecond range.

Diazirine linkers have emerged as a crucial tool in pharmaceutical research and development due to their ability to covalently link small molecules to their binding partners in a photo-activated manner. These photoreactive linkers are characterized by a three-membered diazirine ring that undergoes ring-opening upon exposure to ultraviolet (UV) light, leading to the formation of a highly reactive carbene intermediate. This carbene intermediate can then react with neighboring molecules, enabling the covalent attachment of the small molecule to its binding partner.

Diazirine linkers have found widespread use in drug discovery, as they allow for the identification of protein targets of small molecules through photoaffinity labeling using photo reactive crosslinkers. This technique involves the covalent attachment of a diazirine-containing small molecule to its target protein, followed by UV irradiation to form a covalent bond between the two molecules. This enables the identification and isolation of the protein target, which can then be further characterized and studied.

Furthermore, diazirine linkers have been employed in the development of novel therapeutics, including photoactivatable prodrugs, which are designed to release their active pharmaceutical ingredient upon exposure to UV light. Additionally, diazirine linkers have been used in the design of photoresponsive biomaterials, which can undergo controlled changes in structure and function upon exposure to light. These photoactivated crosslinkers are essential for photo induced cross linking applications, making them invaluable in modern pharmaceutical research.

Diazirine Linkers

Cat# Name Structure M.W. Purity Pricing
AP110162-(3-Methyl-3H-diazirin-3-yl)ethan-1-amine99.13≥95% Pricing
AP110172-(3-Methyl-3H-diazirin-3-yl)ethanol100.12≥95% Pricing
AP110183-methyl-3H-diazirin-3-propanol114.15≥95% Pricing
AP110103-(3-Methyl-3H-diazirin-3-yl)propanoic acid128.13≥95% Pricing
AP150932-[3-(but-3-yn-1-yl)-3H-diazirin-3-yl]ethan-1-amine137.19≥95% Pricing
AP110152-(3-But-3-ynyl-3H-Diazirin-3-yl)-ethanol138.17≥95% Pricing
AP150913-[3-(but-3-yn-1-yl)-3H-diazirin-3-yl]propanenitrile147.18≥95% Pricing
AP150943-(2-azidoethyl)-3-(but-3-yn-1-yl)-3H-diazirine163.18≥95% Pricing
AP110113-[3-(but-3-yn-1-yl)-3H-diazirin-3-yl]propanoic acid166.18≥95% Pricing
AP130683-(2-Iodoethyl)-3-methyl-3H-diazirine210.02≥95% Pricing
AP11020(4-(3-(Trifluoromethyl)-3H-diazirin-3-yl)phenyl)methanamine215.18≥95% Pricing
AP11019{4-[3-(trifluoromethyl)-3H-diazirin-3-yl]phenyl}methanol216.16≥95% Pricing
AP110124-[3-(Trifluoromethyl)-3H-diazirin-3-yl]benzoic acid230.14≥95% Pricing
AP150923-(but-3-yn-1-yl)-3-(2-iodoethyl)-3H-diazirine248.07≥95% Pricing
AP110144-[3-(Trifluoromethyl)-3H-diazirin-3-yl]benzyl Bromide279.06≥95% Pricing
AP11013Benzoic acid, 4-[3-(trifluoromethyl)-3H-diazirin-3-yl] NHS327.22≥95% Pricing
AP11059Diazo Biotin-PEG3-alkyne795.95≥95% Pricing

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