Chemical Name: 1-Methyl-N-[2-methyl-4-[2-(2-methylphenyl)diazenyl]phenyl-1H-pyrazole-5-carboxamide
Biological ActivityPotent aryl hydrocarbon receptor (AhR) antagonist (IC50 = 30 nM). Exhibits no AhR agonist-like activity (at concentrations up to 100 μM). Inhibits 2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD)-induced AhR-dependent transcription in vitro and reduces TCDD-induced toxicity in vivo. Attenuates Th17 differentiation of naive CD4 T cells and promotes expansion of hematopoietic stem cells in vitro.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
CXCR4 activation maintains a stem cell population in tamoxifen-resistant breast cancer cells through AhR signalling.
Dubrovska A, Hartung A, Bouchez LC
Br. J. Cancer, 2012;107(1):43-52.
Aryl hydrocarbon receptor antagonists promote the expansion of human hematopoietic stem cells.
Boitano et al.
Novel compound 2-methyl-2H-pyrazole-3-carboxylic acid (2-methyl-4-o-tolylazo-phenyl)-amide (CH-223191) prevents 2,3,7,8-TCDD-induced toxicity by antagonizing the aryl hydrocarbon receptor.
Kim et al.
Natural agonists for aryl hydrocarbon receptor in culture medium are essential for optimal differentiation of TH17 T cells.
Veldhoen et al.
Citations for CH 223191
The citations listed below are publications that use Tocris products. Selected citations for CH 223191 include:
4 Citations: Showing 1 - 4
Effects of Cigarette Smoke Condensate on Oxidative Stress, Apoptotic Cell Death, and HIV Replication in Human Monocytic Cells.
Authors: Rao Et al.
PLoS One 2016;11:e0155791
A TDO2-AhR Signaling Axis Facilitates Anoikis Resistance and Metastasis in Triple-Negative Breast Cancer.
Authors: D'Amato Et al.
Cancer Res 2015;75:4651
IDO1 suppresses inhibitor development in hemophilia A treated with factor VIII.
Authors: Matino Et al.
Br J Pharmacol 2015;125:3766
Regulation of plasmacytoid dendritic cell development in mice by aryl hydrocarbon receptor.
Authors: Liu Et al.
Immunol Cell Biol 2014;92:200
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Compound purity was as described. Efficacy in assays matched previously published results.
Dissolved in DMSO, avoid freeze/thawing.