ITE |
Catalog No.GC12628
One-Click Copy Product Info
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ITE is an effective immunosuppressive endogenous aromatic hydrocarbon receptor (AhR) agonist, with a Ki value of 3nM for binding to AHR.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 448906-42-1
Sample solution is provided at 25 µL, 10mM.
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ITE is an effective immunosuppressive endogenous aromatic hydrocarbon receptor (AhR) agonist, with a Ki value of 3nM for binding to AhR [1]. AhR is a ligand-dependent transcription factor that mediates the toxicity of several xenobiotics and plays important physiological roles in differentiation, reproduction, and immunity [2]. ITE has immunomodulatory and anti-cancer effects [3-4].
In vitro, ITE (0.1–5000nM; 1-6 days) treatment inhibited the proliferation and migration of ovarian cancer cells (SKOV-3, OVCAR-3, and IOSE-385) in a dose- and time-dependent manner, reduced AhR, and increased CYP1A1 levels [5]. ITE (0.01, 0.1, 1, 5, 10, and 20μM; 2, 4, or 6 days) could inhibit the proliferation of human pulmonary artery endothelial cells (HPAEC) in a dose- and time-dependent manner, reduced AhR protein levels, and simultaneously increased the mRNA levels of cytochrome P450 (CYP), CYP1A1, and CYP1B1 [6].
In vivo, ITE (200μg/0.2mL/day; 14 days; i.p.) treatment could significantly inhibit retinal detachment and ocular inflammatory cell infiltration in mice with experimental autoimmune uveitis (EAU) induced by Freund's adjuvant and Mycobacterium tuberculosis, reduced the proportion of IFN-γ, IL-17, or IL-10 cells in mice, and inhibited the secretion of inflammatory cytokines by mouse lymphocytes [7]. ITE (80mg/kg/day; 28 days; i.p.) treatment could reduce tumor growth by 39% in OVCAR-3 xenograft model mice [5].
References:
[1] Song J, et al. A ligand for the aryl hydrocarbon receptor isolated from lung. Proc Natl Acad Sci U S A. 2002 Nov 12;99(23):14694-9.
[2] Henry E C, Welle S L, Gasiewicz T A. TCDD and a putative endogenous AhR ligand, ITE, elicit the same immediate changes in gene expression in mouse lung fibroblasts[J]. Toxicological Sciences, 2010, 114(1): 90-100.
[3] Dolciami D, Gargaro M, Cerra B, et al. Binding mode and structure–activity relationships of ITE as an aryl hydrocarbon receptor (AhR) agonist[J]. ChemMedChem, 2018, 13(3): 270-279.
[4] Simpson S R, Middleton D D, Lukesh N R, et al. Microparticles incorporating dual apoptotic factors to inhibit inflammatory effects in macrophages[J]. Journal of Pharmaceutical Sciences, 2024, 113(11): 3196-3205.
[5] Wang K, Li Y, Jiang YZ, et al. An endogenous aryl hydrocarbon receptor ligand inhibits proliferation and migration of human ovarian cancer cells. Cancer Lett. 2013;340(1):63-71.
[6] Pang L, Li Y, Zou Q, et al. ITE inhibits growth of human pulmonary artery endothelial cells[J]. Experimental lung research, 2017, 43(8): 283-292.
[7] Nugent LF, Shi G, Vistica BP, Ogbeifun O, Hinshaw SJ, Gery I. ITE, a novel endogenous nontoxic aryl hydrocarbon receptor ligand, efficiently suppresses EAU and T-cell-mediated immunity. Invest Ophthalmol Vis Sci. 2013 Nov 13;54(12):7463-9.
| Cell experiment [1]: | |
Cell lines | SKOV-3, OVCAR-3, and IOSE-385 cells |
Preparation Method | After 16h (Day 0) of seeding in 96-well plates (1000, 5000, and 5000 cells/well for SKOV-3, OVCAR-3, and IOSE-385, respectively; 6 wells/dose), cells were treated with different concentration of ITE (0.1–5000nM) or DMSO (0.1% v/v) in the complete growth media up to 6 days with daily change of media containing dimethyl sulfoxide (DMSO, the vehicle control) or ITE. At the end of treatment, the number of cells per well was determined using a crystal violet method as described. After treatment, cells were rinsed with PBS (5mM phosphate, 145mM NaCl, 5mM KCl, pH 7.5), fixed in methanol for 15min, air-dried for 5min and stained with 0.1% (w/v) crystal violet for 5min. After staining, wells were rinsed with distilled water, and air dried again. Once dry, cells were solubilized with 2% (w/v) sodium deoxycholate solution for 30min with gentle agitation. Absorbance was measured at 570nm on a microplate reader. |
Reaction Conditions | 0.1–5000nM; 1-6 days |
Applications | The ITE treatment exhibited dose- and time-dependent inhibition of the proliferation and migration of ovarian cancer cells. |
| Animal experiment [1]: | |
Animal models | BALB/c nude mice |
Preparation Method | Each mouse was inoculated subcutaneously at the right flank with 5 × 106 of OVCAR-3 cells. When the tumor volume reached approximately 110mm3, the mice were divided into homogeneous blocks based on their tumor volumes followed by randomly assigning each block into the vehicle control and ITE treatment groups (n = 8/group). The vehicle (DMSO) or ITE (80mg/mL in DMSO) was administered to the mice by i.p. injection once daily for 28 days at a volume of 1mL/kg body weight. After the final injection, mice were given an additional 5 days to further monitor tumor volume, body weight, and other clinical signs. |
Dosage form | 80mg/kg/day; 28 days; i.p. |
Applications | The treatment with ITE was able to reduce tumor growth by 39% in the OVCAR-3 xenograft model mice. |
References: | |
| Cas No. | 448906-42-1 | SDF | |
| Chemical Name | methyl 2-(1H-indole-3-carbonyl)-1,3-thiazole-4-carboxylate | ||
| Canonical SMILES | COC(=O)C1=CSC(=N1)C(=O)C2=CNC3=CC=CC=C32 | ||
| Formula | C14H10N2O3S | M.Wt | 286.3 |
| Solubility | ≥ 28.6mg/mL in DMSO | Storage | Store at RT |
| 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 | 3.4928 mL | 17.4642 mL | 34.9284 mL |
| 5 mM | 698.6 μL | 3.4928 mL | 6.9857 mL |
| 10 mM | 349.3 μL | 1.7464 mL | 3.4928 mL |
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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.
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Quality Control & SDS
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- Purity: >99.00% 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.)