ITE

[Description]:

ITE is a potent endogenous agonist of aryl hydrocarbon receptor (AhR), binding directly to AHR, with a Ki of 3 nM. ITE also has immunosuppressive activity.

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Aryl Hydrocarbon Receptor

Research Areas >> Inflammation/Immunology

[Target]

Ki: 3 nM (AhR)[1]

[In Vitro]

ITE is an endogenous agonist of AhR, binding directly to AHR, with a Ki of 3 nM[1]. ITE (0.03-30 mg/mL) decreases the antigen-specific T-cell proliferative responses[2]. ITE potently inhibits human pulmonary artery endothelial (HPAECs) growth at 10 and 20 µM, but shows no effect at 0.01-5 µM. ITE does not affect cell cycle progress of HPAECs at 10 and 20 µM, or induce expression of cleaved caspase-3 protein in HPAECs at 20 µM. In addition, ITE (20 µM) elevates CYP1A1 and CYP1B1 mRNA levels and decreases the levels of AhR protein in HPAECs[3].

[In Vivo]

ITE (200 μg, i.p.) significantly suppresses the development of experimental autoimmune uveitis (EAU) in mice. ITE reduces the proportions of cells expressing IFN-γ, IL-17, or IL-10 in mice. ITE also suppresses the secretion of inflammatory cytokines by LN cells in mice[2].

[Cell Assay]

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 admin]

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.

[2]. Nugent LF, et al. 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.

[3]. Pang LP, et al. ITE inhibits growth of human pulmonary artery endothelial cells. Exp Lung Res. 2017 Oct;43(8):283-292.

[Related Small Molecules]

[ Density]:
1.427g/cm3

[ Boiling Point ]:
520.4ºC at 760 mmHg

[ Molecular Formula ]:
C₁₄H₁₀N₂O₃S

[ Molecular Weight ]:
286.30600

[ Flash Point ]:
268.5ºC

[ Exact Mass ]:
286.04100

[ PSA ]:
100.29000

[ LogP ]:
2.64200

[ Index of Refraction ]:
1.688

[ Storage condition ]:
2-8℃

[ Hazard Codes ]:
Xi

[ Risk Phrases ]:
R36/37/38

[ Safety Phrases ]:
26-36

[ HS Code ]:
2934100090

[ HS Code ]: 2934100090

[ Summary ]:
2934100090 other compounds containing an unfused thiazole ring (whether or not hydrogenated) in the structure VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:20.0%

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Biological Activity

Chemical & Physical Properties

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