GNF-PF-3777 (8-Nitrotryptanthrin) is a potent humanindoleamine 2,3-dioxygenase2 (hIDO2) inhibitor which significantly reducesIDO2activity withK_iof 0.97 μM.

The typtanthrin derivative GNF-PF-3777 (8-Nitrotryptanthrin; Compound 5i) is found to be a potent hIDO2 inhibitor with superior efficiency far better than that of the most frequently-used inhibitor L-1-MT. The IC₅₀values show that all nine tryptanthrin compounds display hIDO2 inhibitory activities, GNF-PF-3777 demonstrates much stronger inhibition (1.87 μM) than both L-1-MT (82.53 μM) and D-1-MT (262.75 μM). GNF-PF-3777 exhibits significant antitrypanosomal activity with EC₅₀of 0.82 μM^[2]. GNF-PF-3777 (8-Nitrotryptanthrin) has a microplate Alamar Blue assay (MABA) minimum inhibitory concentration (MIC) value of 0.032 μg/mL. GNF-PF-3777 also has a LORA MIC value of 2.4 μg/mL, while the majority of analogues lack LORA activity^[3].

293.23

Solid

C₁₅H₇N₃O₄

77603-42-0

Room temperature in continental US; may vary elsewhere.

DMSO : 6.4 mg/mL(21.83 mM;Need warming)

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