IDO-IN-1 is an indoleamine-2,3-dioxygenase (IDO) inhibitor with IC50 of 59 nM, shows activity in Hela cell (IC50=12 nM).
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Indoleamine 2,3-dioxygenase (IDO) is one of the key heme-containing dioxygenases that catalyze the rate limiting step in the catabolism of the essential amino acid tryptophan to N-formylkynurenine by oxidative cleavage of the indole 2,3 double bond[2]. IDO-IN-1 is an IDO inhibitor with IC50 of 59 nM[3]. C57BL/6 mice bearing GMCSF-secreting B16 tumors were subcutaneously administered with IDO-IN-1 at 25, 50, and 75 mg/kg b.i.d. and 50% tumor growth inhibition was observed at 75 mg/kg[3].
作用机制
IDO-IN-1 bounds to IDO through the oxygen of the hydroxyamidine to the iron of the heme in the ferrous state.
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