Tryptanthrin (Synonyms: NSC 349447) |
Catalog No.GC13402
One-Click Copy Product Info
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inhibitor of Cox-2 and 5-LO
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 13220-57-0
Sample solution is provided at 25 µL, 10mM.
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Tryptanthrin, a weakly basic alkaloid tryptophan derivative originally isolated from the dried roots of medicinal indigo plants, has anti-inflammatory and anticancer activities. And, tryptanthrin blocks 5-lipoxygenase (5-LO) and cyclooxygenase-2 (Cox-2) with IC50 values of 600 and 64 nM, respectively.
5-LO and Cox-2 are involved in cancer pathobiology. 5-LO is expressed by a variety of cancer cells including colon, lung, breast, and prostate and promotes cancer cell growth and neo-angiogenesis. Cox-2, overexpressed in cancer cells, promotes tumorigenesis and induces neo-angiogenesis.
In vitro: In human hepatocyte-derived HepG2 cells, tryptanthrin inhibited the reactive oxygen species formation, mitochondrial dysfunction, and cell death triggered by tert-butyl hydroperoxide (tBHP). Furthermore, tryptanthrin reversed the reduction of glutathione (GSH) induced by tBHP. Specifically, nuclear translocation, transactivation of nuclear factor erythroid 2-related factor 2 (Nrf2), and phosphorylation of extracellular signal-regulated kinase (ERK) were evoked by the treatment of tryptanthrin. Additionally, the expression of the heme oxygenase 1 and glutamate was upregulated by tryptanthrin [1].
In vivo: BALB/c (H-2d) mice, intraperitoneally (i.p.) inoculated with leukemia WEHI-3B JCS cells, were injected i.p with tryptanthrin at doses of 0.04 mg/kg, 0.08 mg/kg and 0.16 mg/kg body weight for 5 consecutive days. Tryptanthrin inhibited the growth of WEHI-3B JCS cells in BALB/c mice, and at the dosages of 0.08 mg/kg and 0.16 mg/kg, significant inhibition was seen. Moreover, tryptanthrin, in a dose-dependent fashion, triggered cell cycle arrest of the WEHI-3B JCS cells at G0/G1 phase [2].
References:
[1]. Moon, S., Lee, J., Choi, H., Cho, I., Kim, S., & Kim, Y. Tryptanthrin Protects Hepatocytes against Oxidative Stress via Activation of the Extracellular Signal-Regulated Kinase/NF-E2-Related Factor 2 Pathway. Biological and Pharmaceutical Bulletin. 2014; 37(10): 1633-1640.
[2]. Chan, H., Yip, H., Mak, N., & Leung, K. Modulatory Effects and Action Mechanisms of Tryptanthrin on Murine Myeloid Leukemia Cells. Cellular and Molecular Immunology. 2009; 6(5): 335-342.
| Cas No. | 13220-57-0 | SDF | |
| Synonyms | NSC 349447 | ||
| Chemical Name | indolo[2,1-b]quinazoline-6,12-dione | ||
| Canonical SMILES | O=C1N2C(C(C3=C2C=CC=C3)=O)=NC4=C1C=CC=C4 | ||
| Formula | C15H8N2O2 | M.Wt | 248.2 |
| Solubility | ≤30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.029 mL | 20.145 mL | 40.2901 mL |
| 5 mM | 805.8 μL | 4.029 mL | 8.058 mL |
| 10 mM | 402.9 μL | 2.0145 mL | 4.029 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)