GNF-PF-3777 (8-Nitrotryptanthrin)
(Synonyms: 8-Nitrotryptanthrin) 目录号 : GC33671A tryptanthrin derivative with diverse biological activities
Cas No.:77603-42-0
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. |
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)
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 |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
||
Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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 |
10 mM | 0.341 mL | 1.7051 mL | 3.4103 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
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.