GNF-PF-3777 (8-Nitrotryptanthrin) 是一种有效的人吲哚胺2，3-双加氧酶 2 (hIDO2) 抑制剂，有效降低 IDO2 活性，K_i 值为 0.97 μM。

GNF-PF-3777 (8-Nitrotryptanthrin) is a potent human indoleamine 2,3-dioxygenase 2 (hIDO2) inhibitor which significantly reduces IDO2 activity with K i of 0.97 μM.

Solid

rhIDO2 1.8 μM (IC50) rhIDO2 0.97 μM (Ki)

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. has not independently confirmed the accuracy of these methods. They are fo

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Li J, et al. Establishment of a human indoleamine 2, 3-dioxygenase 2 (hIDO2) bioassay system and discovery of tryptanthrin derivatives as potent hIDO2 inhibitors. Eur J Med Chem. 2016 Nov 10;123:171-9.
[2]. Scovill J, et al. Antitrypanosomal activities of tryptanthrins. Antimicrob Agents Chemother. 2002 Mar;46(3):882-3.

In Vitro: DMSO : 6.4 mg/mL (21.83 mM; Need warming)配制储备液