GNF-PF-3777

Research use only, not for human use.

GNF-PF-3777 (8-Nitrotryptanthrin) is a potent inhibitor of human indoleamine 2,3-dioxygenase 2.

GNF-PF-3777 (8-Nitrotryptanthrin) is a potent inhibitor of human indoleamine 2,3-dioxygenase 2 (hIDO2; Ki: 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 IC50 values 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 EC50 of 0.82 μM. 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.

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8-Nitrotryptanthrin

Metabolic Enzyme/Protease

IDO

rhIDO2

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77603-42-0

293.23

C15H7N3O4

>98% (HPLC)

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

[O-][N+](c(cc1)cc(C(C2=Nc3c4cccc3)=O)c1N2C4=O)=O

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(-20℃)

With Ice Pack

≥ 2 years