ITE |
| Catalog No.GC12628 |
ITE는 3 nM의 Ki로 AHR에 직접 결합하는 아릴 탄화수소 수용체(AhR)의 강력한 내인성 작용제입니다.
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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2-(1′H-indole-3′-carbonyl)-thiazole-4-carboxylic acid methyl ester (ITE) is a nontoxic immunosuppressive endogenous aryl hydrocarbon receptor (AhR) ligand [1] [2]. Its EC50 identified via yeast AhR assay is 7.8×10−10 mol/l [3].
AhR is a transcription factor mediating toxic effects of environmental pollutants such as 2, 3, 7, 8-tetrachlorodibenzo-p-dioxin (TCDD), it is activated by ligand [2].
ITE inhibited TGFβ1-induced myofibroblast differentiation in TGFβ1-challenged cultures of primary human fibroblasts from several distinct tissue types. In primary human orbital fibroblasts, ITE inhibited TGFβ1-induced nuclear translocation of Smad2/3/4 and its subsequent binding to SBE, but it did not inhibit TGFβ1-induced phosphorylation of Smad2/3, Erk1/2, or Akt [4], it inhibited TGFβ1 (1 ng/mL)-induced α-smooth muscle actin (α-SMA) expression, extracellular matrix production [5]. The inhibition of ITE to TGFβ1-induced myofibroblast differentiation in primary human fibroblasts is AhR independent [5].
In Sprague-Dawley rats maintained under a 12 h light/12 h dark cycle and given free access to a solid diet and distilled water, ITE at 1.6 and 8.0 mg/kg bw, significantly increased the CYP1A1 mRNA levels by 5.59 and 68.55 fold, respectively. It indicated that ITE activated AhR activation in placentas. 8.0 mg/kg bw ITE elevated the level of HIF-1a mRNA, induced the levels of VEGF-A, VEGF-B and PIGF mRNA in a dose-dependent manner [6].
References:
[1]. Lindsey F. Nugent, Guangpu Shi, Barbara P. Vistica, et al. ITE, A Novel Endogenous Nontoxic Aryl Hydrocarbon Receptor Ligand, Efficiently Suppresses EAU and T-Cell–Mediated Immunity. Invest Ophthalmol Vis Sci., 2013, 54(12):7463-7469.
[2]. Jaishree Bankoti, Ben Rase, Tom Simones, et al. Functional and phenotypic effects of AhR activation in inflammatory dendritic cells. Toxicol Appl Pharmacol., 2010, 246(1-2):18-28.
[3]. S. Medjakovic and A. Jungbauer. Red clover isoflavones biochanin A and formononetin are potent ligands of the human aryl hydrocarbon receptor. Journal of Steroid Biochemistry & Molecular Biology, 2008, 108:171-177.
[4]. Geniece M. Lehmann, Xia Xi, Ajit A. Kulkarni, et al. The Aryl Hydrocarbon Receptor Ligand ITE Inhibits TGFβ1-Induced Human Myofibroblast Differentiation. American Journal of Pathology, 2011, 178(4):1556–1567.
[5]. Geniece M. Lehmann, Xia Xi, Ajit A. Kulkarni, et al. The Aryl Hydrocarbon Receptor Ligand ITE Inhibits TGF1-Induced Human Myofibroblast Differentiation. The American Journal of Pathology, 2011, 178(4):1556-1567.
[6]. Yanming Wu, Xiao Chen, Qian Zhou, et al. ITE and TCDD Differentially Regulate the Vascular Remodeling of Rat Placenta via the Activation of AhR. PLoS ONE, 2014, 9(1): e86549.
Cell experiment: | Subconfluent cells (25, 000 cells/well) are seeded in 96-well plates. Cells are treated with ITE at 5, 10 and 20 µM or DMSO (0.1% v/v) in ECM for 2, 4 or 6 days with a change of ECM containing DMSO or ITE every other day (5 wells/treatment). At the end of treatment, cells are incubated with MTT reagent for 4 hr, and solubilized in crystal dissolving solution (100 µL/well) for 20 min. The absorbance is determined at 570 nm using the microplate reader[3]. |
Animal experiment: | Mice[2]Eight- to 12-week-old female B10.A mice is used in the assay. Daily treatment starts on day 0 and consists of 200 μg of ITE suspended in 0.2 mL PBS, given intraperitoneally. Control mice are similarly treated with 0.2 mL of the vehicle, PBS containing 3.6% DMSO[2]. |
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. | |
| 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 | 0.6986 mL | 3.4928 mL | 6.9857 mL |
| 10 mM | 0.3493 mL | 1.7464 mL | 3.4928 mL |
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Quality Control & SDS
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- Purity: >99.00%
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Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)
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