DDD85646 (Synonyms: IMP-366) |
| Catalog No.GC43386 |
DDD85646 est un puissant inhibiteur de la N-myristoyltransférase de trypanosoma brucei (TbNMT IC50 = 2 nm ; hNMTIC50 = 4 nm).
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Cas No.: 1215010-55-1
Sample solution is provided at 25 µL, 10mM.
DDD85646 is a moderately bioavailable pyrazole sulphonamide inhibitor of T. brucei N-myristoyltransferase (TbNMT) with an apparent Ki value of 1.44 nM.1 T. brucei is the parasite responsible for human African trypanosomiasis (HAT), also known as African sleeping sickness, and is transmitted through the tsetse fly. DDD85646 administration in mice (12.5 mg/kg for four days) ameliorated T. brucei in an acute mouse model of HAT.[1] It less potently inhibits growth of T. cruzi (EC50 = 6.9 µM).
Reference:
1. Frearson, J.A., Brand, S., McElroy, S.P., et al. N-myristoyltransferase inhibitors as new leads to treat sleeping sickness. Nature 464(7829), 728-732 (2010).
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
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