Wilkinson, Isabel V. L.; Reynolds, Jessica K.; Galan, Sebastien R. G.; Vuorinen, Aini; Sills, Adam J.; Pires, Elisabete; Wynne, Graham M.; Wilson, Francis X.; Russell, Angela J. published the artcile< Characterisation of utrophin modulator SMT C1100 as a non-competitive inhibitor of firefly luciferase>, HPLC of Formula: 115144-35-9, the main research area is firefly luciferase bioluminescence enzyme kinetics inhibitor duchenne muscular dystrophy; Assay interference; Bioluminescence; Duchenne muscular dystrophy; Enzyme inhibitor; Enzyme kinetics; Enzyme mechanism; Firefly luciferase; Inhibition mechanism; Photoaffinity probe.
Firefly luciferase (FLuc) is a powerful tool for mol. and cellular biol., and popular in high-throughput screening and drug discovery. However, FLuc assays have been plagued with pos. and neg. artifacts due to stabilization and inhibition by small mols. from a range of chem. classes. Here we disclose Phase II clin. compound SMT C1100 for the treatment of Duchenne muscular dystrophy as an FLuc inhibitor (KD of 0.40 ± 0.15μM). Enzyme kinetic studies using SMT C1100 and other non-competitive inhibitors including resveratrol and NFκBAI4 identified previously undescribed modes of inhibition with respect to FLuc’s luciferyl adenylate intermediate. Employing a photoaffinity strategy to identify SMT C1100’s binding site, a photolabeled SMT C1100 probe instead underwent FLuc-dependent photooxidation Our findings support novel binding sites on FLuc for non-competitive inhibitors.
Bioorganic Chemistry published new progress about Chemiluminescent probes. 115144-35-9 belongs to class thiazole, and the molecular formula is C11H7KN2O3S2, HPLC of Formula: 115144-35-9.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica