NMT-IN-1 is a Trypanosoma brucei N-myristoyltransferase (TbNMT) inhibitor, with an IC50 of 31 µM against TbNMT and an IC50 of 66 µM against hNMT. As a thiazolidinone hit compound identified via virtual screening, NMT-IN-1 exerts enzymatic inhibitory effects by binding to the active site of TbNMT. NMT-IN-1 adopts a binding mode distinct from that of pyrazole sulfonamide inhibitors and can inhibit the myristoyl transfer reaction catalyzed by TbNMT. NMT-IN-1 is mainly used in the research of anti-parasitic lead compounds for human African trypanosomiasis (African sleeping sickness). It provides a structural basis for the subsequent optimization of TbNMT inhibitors with high activity, high selectivity and blood-brain barrier permeability.[1]
Molekulargewicht:
270.35
Reinheit:
98
CAS Nummer:
[326879-46-3]
Formel:
C15H14N2OS
Target-Kategorie:
Parasite
Anwendungsbeschreibung:
MCE Product type: Reference compound1
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