GNF-PF-3777
Based on 2 publication(s) in Google Scholar
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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98.03%
- CAS 番号: 77603-42-0
- 分子式: C15H7N3O4
- 分子量:293.23
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 GNF-PF-3777
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生物活性
製品説明
IC50 & Target
[1]|
rhIDO2 1.8 μM (IC50) |
rhIDO2 0.97 μM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A498 | GI50 |
2 μM
Compound: 7
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Tested for in vitro cytotoxic activity against renal A498 human cancer cell lines
Tested for in vitro cytotoxic activity against renal A498 human cancer cell lines
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[PMID: 12161121] |
| A498 | GI50 |
3 μM
Compound: 10a
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Growth inhibition of human A498 cells assessed as reduction in cell viability
Growth inhibition of human A498 cells assessed as reduction in cell viability
|
[PMID: 38665827] |
| A549 | IC50 |
6.88 μM
Compound: 10a
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Antiproliferative activity against human A549 cells incubated by 48 hrs by MTT assay
Antiproliferative activity against human A549 cells incubated by 48 hrs by MTT assay
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[PMID: 38665827] |
| B16-F10 | IC50 |
0.49 μM
Compound: 10a
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Antiproliferative activity against mouse B16-F10 cells
Antiproliferative activity against mouse B16-F10 cells
|
[PMID: 38665827] |
| DU-145 | GI50 |
0.15 μM
Compound: 10a
|
Growth inhibition of human DU-145 cells assessed as reduction in cell viability
Growth inhibition of human DU-145 cells assessed as reduction in cell viability
|
[PMID: 38665827] |
| DU-145 | GI50 |
8 μM
Compound: 7
|
Tested for in vitro cytotoxic activity against prostate DU145 human cancer cell lines
Tested for in vitro cytotoxic activity against prostate DU145 human cancer cell lines
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[PMID: 12161121] |
| HEK293 | IC50 |
0.018 nM
Compound: 5i
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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
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[PMID: 24099220] |
| HEK293 | IC50 |
0.061 μM
Compound: 5i
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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] |
| HeLa | IC50 |
0.34 μM
Compound: 10a
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Antiproliferative activity against human HeLa cells
Antiproliferative activity against human HeLa cells
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[PMID: 38665827] |
| Hep 3B2 | IC50 |
1.4 μM
Compound: 10a
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Anticancer activity against human Hep3B cells measured after 48 hrs
Anticancer activity against human Hep3B cells measured after 48 hrs
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[PMID: 38665827] |
| HepG2 | IC50 |
7.89 μM
Compound: 10a
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Antiproliferative activity against human HepG2 cells incubated by 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells incubated by 48 hrs by MTT assay
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[PMID: 38665827] |
| Huh-7 | CC50 |
>10 μM
Compound: GNF-Pf-3777
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NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
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[PMID: 18579783] |
| K562 | IC50 |
8.05 μM
Compound: 10a
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Antiproliferative activity against human K562 cells incubated by 48 hrs by MTT assay
Antiproliferative activity against human K562 cells incubated by 48 hrs by MTT assay
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[PMID: 38665827] |
| LX-2 | IC50 |
0.83 μM
Compound: 10a
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Antiproliferative activity against human LX-2 cells
Antiproliferative activity against human LX-2 cells
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[PMID: 38665827] |
| M14 | GI50 |
0.8 μM
Compound: 10a
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Growth inhibition of human M14 cells assessed as reduction in cell viability
Growth inhibition of human M14 cells assessed as reduction in cell viability
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[PMID: 38665827] |
| M14 | GI50 |
15 μM
Compound: 7
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Tested for in vitro cytotoxic activity against melanoma M14 human cancer cell lines
Tested for in vitro cytotoxic activity against melanoma M14 human cancer cell lines
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[PMID: 12161121] |
| NCI/ADR-RES | GI50 |
0.7 μM
Compound: 10a
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Growth inhibition of human MCF7ADR cells assessed as reduction in cell viability
Growth inhibition of human MCF7ADR cells assessed as reduction in cell viability
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[PMID: 38665827] |
| NCI/ADR-RES | GI50 |
1 μM
Compound: 7
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Tested for in vitro cytotoxic activity against breast MCF-7/ADR human cancer cell lines
Tested for in vitro cytotoxic activity against breast MCF-7/ADR human cancer cell lines
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[PMID: 12161121] |
| NCI-H522 | GI50 |
0.7 μM
Compound: 10a
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Growth inhibition of human NCI-H522 cells assessed as reduction in cell viability
Growth inhibition of human NCI-H522 cells assessed as reduction in cell viability
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[PMID: 38665827] |
| NCI-H522 | GI50 |
4.8 μM
Compound: 7
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Tested for in vitro cytotoxic activity against lung H522 human cancer cell lines
Tested for in vitro cytotoxic activity against lung H522 human cancer cell lines
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[PMID: 12161121] |
| PC-3 | IC50 |
11.83 μM
Compound: 10a
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Antiproliferative activity against human PC-3 cells incubated by 48 hrs by MTT assay
Antiproliferative activity against human PC-3 cells incubated by 48 hrs by MTT assay
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[PMID: 38665827] |
| SK-OV-3 | GI50 |
25 μM
Compound: 7
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Tested for in vitro cytotoxic activity against ovarian SKOV3 human cancer cell lines
Tested for in vitro cytotoxic activity against ovarian SKOV3 human cancer cell lines
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[PMID: 12161121] |
| SK-OV-3 | GI50 |
5 μM
Compound: 10a
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Growth inhibition of human SK-OV-3 cells assessed as reduction in cell viability
Growth inhibition of human SK-OV-3 cells assessed as reduction in cell viability
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[PMID: 38665827] |
| SW-620 | GI50 |
25 μM
Compound: 7
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Tested for in vitro cytotoxic activity against colon SW620 human cancer cell lines
Tested for in vitro cytotoxic activity against colon SW620 human cancer cell lines
|
[PMID: 12161121] |
| SW-620 | GI50 |
4 μM
Compound: 10a
|
Growth inhibition of human SW620 cells assessed as reduction in cell viability
Growth inhibition of human SW620 cells assessed as reduction in cell viability
|
[PMID: 38665827] |
| U-251 | GI50 |
>100 μM
Compound: 10a
|
Growth inhibition of human U-251 cells assessed as reduction in cell viability
Growth inhibition of human U-251 cells assessed as reduction in cell viability
|
[PMID: 38665827] |
| U-251 | GI50 |
4.5 μM
Compound: 7
|
Tested for in vitro cytotoxic activity against CNS U251 human cancer cell lines
Tested for in vitro cytotoxic activity against CNS U251 human cancer cell lines
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[PMID: 12161121] |
| 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
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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] |
| Vero | IC50 |
28 μg/mL
Compound: 1b
|
Cytotoxicity against african green monkey Vero cells
Cytotoxicity against african green monkey Vero cells
|
[PMID: 23360475] |
体外実験
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.
化学情報
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CAS 番号 77603-42-0
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性状 Solid
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分子量 293.23
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分子式 C15H7N3O4
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Color White to off-white
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SMILES
O=C1N2C(C(C3=C2C=CC([N+]([O-])=O)=C3)=O)=NC4=CC=CC=C41
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別名
8-Nitrotryptanthrin
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Chem Biol
2023 Aug 17;30(8):987-998.e24. PMID: 37490918 -
溶剤 & 溶解度
体外:
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[2]. Scovill J, et al. Antitrypanosomal activities of tryptanthrins. Antimicrob Agents Chemother. 2002 Mar;46(3):882-3. [Content Brief]
[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. [Content Brief]
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 |
GNF-PF-3777 関連分類
HY-100687 関連分類
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