2. Metabolic Enzyme/Protease
  3. Indoleamine 2,3-Dioxygenase (IDO)
  4. GNF-PF-3777

GNF-PF-3777  (Synonyms: 8-Nitrotryptanthrin)

Cat. No.: HY-100687 Purity: 98.03%
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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.

For research use only. We do not sell to patients.

GNF-PF-3777 Chemical Structure

GNF-PF-3777 Chemical Structure

CAS No. : 77603-42-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 319 In-stock
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10 mM * 1 mL in DMSO USD 319 In-stock
Solid
1 mg USD 98 In-stock
5 mg USD 216 In-stock
10 mg USD 325 In-stock
25 mg USD 586 In-stock
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Based on 1 publication(s) in Google Scholar

GNF-PF-3777 Related Antibodies

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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.

IC50 & Target[1]

rhIDO2

1.8 μM (IC50)

rhIDO2

0.97 μM (Ki)

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.018 nM
Compound: 5i
Inhibition of human IDO1 expressed in HEK293 cells assessed as kynurenine release after 5 hrs by spectrophotometry
Inhibition of human IDO1 expressed in HEK293 cells assessed as kynurenine release after 5 hrs by spectrophotometry
[PMID: 24099220]
HEK293 IC50
0.061 μM
Compound: 5i
Inhibition of TDO (unknown origin) expressed in HEK293 cells using L-Trp as substrate after 8 hrs
Inhibition of TDO (unknown origin) expressed in HEK293 cells using L-Trp as substrate after 8 hrs
[PMID: 30321802]
U-87MG ATCC IC50
0.04 μM
Compound: 5i
Inhibition of TDO in human U87 MG cells using L-Trp as substrate after 8 hrs
Inhibition of TDO in human U87 MG cells using L-Trp as substrate after 8 hrs
[PMID: 30321802]
U-87MG ATCC IC50
0.45 μM
Compound: 5i
Inhibition of recombinant human IDO2 expressed in human U87MG cells assessed as reduction in kynurenine formation using L-tryptophan as substrate after 6 hrs by spectrophotometry
Inhibition of recombinant human IDO2 expressed in human U87MG cells assessed as reduction in kynurenine formation using L-tryptophan as substrate after 6 hrs by spectrophotometry
[PMID: 27475108]
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[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GNF-PF-3777 Related Antibodies
Molecular Weight

293.23

Formula

C15H7N3O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N2C(C(C3=C2C=CC([N+]([O-])=O)=C3)=O)=NC4=CC=CC=C41
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 6.4 mg/mL (21.83 mM; Need warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4103 mL 17.0515 mL 34.1029 mL
5 mM 0.6821 mL 3.4103 mL 6.8206 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References
Cell Assay
[1]

To study the cellular hIDO2 inhibition of candidate compounds, recombinant plasmid pcDNA3.1(+)-hIDO2 is constructed and transfected into human glioblastoma U87 MG cells which had no IDO1 expression (confirmed by RT-PCR and western blot) therefore eliminated the interference of IDO1. U87 MG cells are cultivated in DMEM containing 50 U/mL penicillin, 50 mg/mL streptomycin, 4500 mg/L glucose, and 10% inactivated FBS at 37°C with 5% CO2 and 95% humidity. When a cell density of 80% confluent monolayer is reached, U87 MG cells are transfected with pcDNA3.1(+)-hIDO2 using the transfection reagent Lipofectamine 2000 according to the manufacturer's instructions. An empty pcDNA3.1(+) expression vector is served as control. After 18 h of incubation, the transfected cells are seeded in 96-well culture plates at a density of 2.5×104 cells/well in a final volume of 200 μL supplemented with 200 μM L-Trp. A serial dilution of the tested compounds is added to the culture medium after an additional 6 h of incubation. The reaction is terminated by addition of 30% (w/v) trichloroacetic acid (10 μL for 140 μL of the reaction mixture) 24 h later. The plates are incubated at 65°C in water bath for 15 min to facilitate the transformation of N-formylkynurenine to L-kynurenine, followed by centrifugation at 13,000× g for 10 min to remove the sediments. 100 μL of the supernatant are then transferred to another 96-well plate and mixed with a same volume of 2% (w/v) 4-dimethylaminobenzaldehyde in acetic acid. The percentages of inhibition of tryptophan degradation or kynurenine production by the compounds are calculated by measuring the absorption at 492 nm using a microplate reader. Cellular IC50s are determined via non-linear regression analysis using GraphPad Prism 5.0[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4103 mL 17.0515 mL 34.1029 mL 85.2573 mL
5 mM 0.6821 mL 3.4103 mL 6.8206 mL 17.0515 mL
10 mM 0.3410 mL 1.7051 mL 3.4103 mL 8.5257 mL
15 mM 0.2274 mL 1.1368 mL 2.2735 mL 5.6838 mL
20 mM 0.1705 mL 0.8526 mL 1.7051 mL 4.2629 mL
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GNF-PF-3777 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GNF-PF-377777603-42-08-NitrotryptanthrinIndoleamine 2,3-Dioxygenase (IDO)Inhibitorinhibitorinhibit

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