photoaffinity

YM 534 has antitumor activity and platelet aggregation activity, inhibits photoaffinity labeling of deglycosylated P-glycoprotein, and can be used to study leukemia.

PARPYnD is a potent photoaffinity probe for poly(ADP-ribose) polymerase (PARP) (IC50 values for PARP2, PARP1 and PARP6 are 6, 38 and 230 nM, respectively). PARPYnD labels PARP1 and PARP2 in the cell when an N3 functionalized fluorescent probe is attached and can inhibit isolated PARP6.

Nitrobenzylthioinosine (NBMPR) is an inhibitor of ENT1 transporter that binds to ENT1 transporter with high affinity.

Azidothiorphan is a photoaffinity ligand for the active site of the neutral endopeptidase 24.11. After ultraviolet irradiation the inhibitor binds irreversibly to the enzyme, and photolabeling occurs at the active site. The competitive inhibitor thiorphan protects the endopeptidase from inactivation.

RO-57-Bpyne is a γ-secretase modulator photoaffinity probe. It also can be exploited to reduce levels of pathogenic Aβ species. It acts by identifying distinct allosteric binding sites on presenilin.

2,6-Dichloropurine-9-β-D-riboside is a building block.1,2It has been used in the synthesis of photoaffinity probes for nucleotide binding sites in proteins. 1.Wower, J., Hixson, S.S., Sylvers, L.A., et al.Synthesis of 2,6-diazido-9-(β-D-ribofuranosyl)purine 3',5'-bisphosphate: Incorporation into transfer RNA and photochemical labeling of Escherichia coli ribosomesBioconjug. Chem.5(2)158-161(1994) 2.Seiter, M.S., Bauer, M.P., Bogel, P.D., et al.Synthesis of novel spin-labeled photoaffinity derivatives of NAD+ and ATP and their characterization as coenzymes and substrates of several enzymesSynthesis2269-273(1996)

Antibacterial agent 116, a benzophenone-containing salicylanilide compound, exhibits potent antibacterial activity by inhibiting peptidoglycan formation. It is employed as a photoaffinity probe to label Acinetobacter baumannii penicillin-binding protein (PBP1b), thereby blocking the propagation pathway and disrupting the growth of the peptidoglycan chain.

163-bp3 is an effective photoaffinity probe and can be used as a target γ Secretory enzyme.

L458-BPyne is a γ-secretase modulator photoaffinity probe that acts by identifying distinct allosteric binding sites on presenilin. It also can be exploited to reduce levels of pathogenic Aβ species.

Nph-peptide can be used for photoaffinity labeling of the N-formyl peptide receptor site of intact human polymorphonuclear leukocytes.

L 669083 is two classes of potent leukotriene biosynthesis inhibitors photoaffinity analogue.

Fmoc-L-photo-proline is an amino acid capable of photo-crosslinking, designed for incorporation into synthetic peptides through solid-phase Fmoc chemistry. It facilitates the synthesis of cyclic peptidomimetic antibiotics and is utilized in the preparation of a wide array of peptide-based photoaffinity probes for research purposes [1].

LU 49888 is a photoaffinity analog of verapamil that has been used to identify specific binding sites for phenylalkylamines of calcium channels present in rabbit skeletal muscle microsomes.

Benzoylphenylalanine (LBPA) can be used as a photoaffinity peptide inactivator.

CGP 55802A is a novel photoaffinity ligand for in-situ labeling of NMDA receptors.

GNF351 is a full antagonist of the aryl hydrocarbon receptor (AHR)with the capacity to inhibit both DRE-dependent and -independent activity. GNF351 is minimal toxicity in mouse or human keratinocytes. GNF351 competes with a photoaffinity AHR ligand for binding to the AHR (IC50: 62 nM).

BI-RJ 70 is a tritiated photoaffinity azide analog of nevirapine, which can be used to study the binding of nevirapine to HIV-1 transcriptase through covalently labeled enzymes and amino acid residues.

4-Azido-L-phenylalanine (p-Azido-L-phenylalanine) is an amino acid derivative that acts as a photoaffinity marker and can be used to detect localized protein environments.