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Compounds that are analog of macrolides that contain lactam rings in place of lactone rings; they are a class of antibiotics. Lactam rings are nitrogen analogs of lactone rings.
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Tacrolimus anhydrous 8-epimer (Tacrolimus EP impurity D) is a l-pipecolic acid macrolide lactone an important immunosuppressive agent that blocks T cell proliferation in vitro by inhibiting the generation of several lymphokines especially IL-2[1]
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FK 866 hydrochloride (CAS 658084-64-1 free base) is a potent inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase) an enzyme essential for NAD biosynthesis exhibiting activity with IC50 values ranging from 0 09 nM to 27 2 nM By blocking NAD synthesis FK 866 disrupts ATP production induces mitochondria membrane depolarization and triggers autophagy independent of caspase activation It selectively targets hematologic cancer cells such as AML lines sparing normal hematopoietic progenitor cells FK 866 demonstrates antitumor efficacy in vivo significantly suppressing growth in AML-M4 and Namalwa xenograft models
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