| ITEAHR agonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 98.07%
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| Cas No. | 448906-42-1 | SDF | Download 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 |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
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