Description
GNF-PF-3777 (8-Nitrotryptanthrin) is a potent human indoleamine 2,3-dioxygenase 2 (hIDO2) inhibitor which significantly reduces IDO2 activity with Ki of 0.97 μM.
Product information
CAS Number: 77603-42-0
Molecular Weight: 293.23
Formula: C15H7N3O4
Chemical Name: 8-nitro-6H,12H-indolo[2,1-b]quinazoline-6,12-dione
Smiles: [O-][N+](=O)C1=CC2=C(C=C1)N1C(=NC3=CC=CC=C3C1=O)C2=O
InChiKey: UFMQJYHLIUACCG-UHFFFAOYSA-N
InChi: InChI=1S/C15H7N3O4/c19-13-10-7-8(18(21)22)5-6-12(10)17-14(13)16-11-4-2-1-3-9(11)15(17)20/h1-7H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 6.4 mg/mL (21.83 mM; Need warming).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
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.
Products are for research use only. Not for human use.
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