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GNF-PF-3777 (8-Nitrotryptanthrin) Sale

(Synonyms: 8-Nitrotryptanthrin) 目录号 : GC33671

A tryptanthrin derivative with diverse biological activities

GNF-PF-3777 (8-Nitrotryptanthrin) Chemical Structure

Cas No.:77603-42-0

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥2,610.00
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1mg
¥810.00
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5mg
¥2,250.00
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10mg
¥3,420.00
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50mg
¥9,450.00
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100mg
¥14,850.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment:

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].

References:

[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.
[3]. Hwang JM, et al. Design, synthesis, and structure-activity relationship studies of tryptanthrins as antitubercular agents. J Nat Prod. 2013 Mar 22;76(3):354-67.

产品描述

8-Nitrotryptanthrin is a derivative of tryptanthrin with diverse biological activities.1,2,3,4,5 It inhibits human recombinant indoleamine 2,3-dioxygenase 1 (IDO1; IC50 = 0.103 μM) and its enzyme activity in HEK293 cells expressing human IDO1 (IC50 = 0.18 μM).1 8-Nitrotryptanthrin inhibits the growth of U251 glioblastoma, H522 lung, M14 melanoma, DU145 prostate, and A498 renal cancer cells (GI50s = 4.5, 4.8, 15, 8, and 2 μM, respectively).2 It is active against M. tuberculosis, methicillin resistant S. aureus (MRSA), and M. furfur (MICs = 0.032, 0.5, and 5 μg/ml, respectively).3,4 8-Nitrotyrptanthrin is also active against T. brucei (EC50 = 0.24 μg/ml).5

1.Yang, S., Li, X., Hu, F., et al.Discovery of tryptanthrin derivatives as potent inhibitors of indoleamine 2,3-dioxygenase with therapeutic activity in Lewis lung cancer (LLC) tumor-bearing miceJ. Med. Chem.56(21)8321-8331(2013) 2.Sharma, V.M., Prasanna, P., Seshu, K.V., et al.Novel indolo[2,1-b]quinazoline analogues as cytostatic agents: Synthesis, biological evaluation and structure-activity relationshipBioorg. Med. Chem. Lett.12(17)2303-2307(2002) 3.Hwang, J.-M., Oh, T., Kaneko, T., et al.Design, synthesis, and structure-activity relationship studies of tryptanthrins as antitubercular agentsJ. Nat. Prod.76(3)354-367(2013) 4.Kawakami, J., Matsushima, N., Ogawa, O., et al.Antibacterial and antifungal activities of tryptanthrin derivativesTrans. Mater. Res. Soc. Jpn.36(4)603-606(2011) 5.Scovill, J., Blank, E., Konnick, M., et al.Antitrypanosomal activities of tryptanthrinsAntimicrob. Agents Chemother.46(3)882-883(2002)

Chemical Properties

Cas No. 77603-42-0 SDF
别名 8-Nitrotryptanthrin
Canonical SMILES O=C1N2C(C(C3=C2C=CC([N+]([O-])=O)=C3)=O)=NC4=CC=CC=C41
分子式 C15H7N3O4 分子量 293.23
溶解度 DMSO : 6.4 mg/mL (21.83 mM) 储存条件 Store at -20°C
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溶解性数据

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1 mM 3.4103 mL 17.0515 mL 34.1029 mL
5 mM 0.6821 mL 3.4103 mL 6.8206 mL
10 mM 0.341 mL 1.7051 mL 3.4103 mL
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Research Update

Axl, Immune Checkpoint Molecules and HIF Inhibitors from the Culture Broth of Lepista luscina

Molecules 2022 Dec 15;27(24):8925.PMID:36558053DOI:PMC9781456

Two compounds 1 and 2 were isolated from the culture broth of Lepista luscina. This is the first time that compound 1 was isolated from a natural source. The structure of compound 1 was identified via 1D and 2D NMR and HRESIMS data. Compounds 1 and 2 along with 8-Nitrotryptanthrin (4) were evaluated for their biological activities using the A549 lung cancer cell line. As a result, 1 and 2 inhibited the expression of Axl and immune checkpoint molecules. In addition, compounds 1, 2 and 4 were tested for HIF inhibitory activity. Compound 2 demonstrated statistically significant HIF inhibitory effects on NIH3T3 cells and 1 and 2 against ARPE19 cells.