Chemical Name: 3-(1,3-Benzodioxol-5-yl)-1-(cis-3,5-dimethyl-1-piperidinyl)-3-(2-hydroxy-4,6-dimethoxyphenyl)-1-propanone
Biological Activity(±)-ML 209 is a RORγt inverse agonist (IC50 = 460 nM). Suppresses Th17 cell differentiation and IL17A expression in vitro. Does not suppress transcription of RORα. Minimal activity displayed on ERα, LXRα and thyroid hormone receptors (IC50 values >4.4 μM).
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Tocris products are intended for laboratory research use only, unless stated otherwise.
DDX5 and its associated lncRNA Rmrp modulate TH17 cell effector functions.
Huang et al.
REV-ERB and ROR nuclear receptors as drug targets.
Kojetin et al.
Nat.Rev.Drug Discov., 2014;13:197
Identification of Potent and Selective RORγ Antagonists.
Huang et al.
Probe Reports from the NIH Molecular Libraries Program, 2010;
Discovery of novel N-(5-(arylcarbonyl)thiazol-2-yl)amides and N-(5-(arylcarbonyl)thiophen-2-yl)amides as potent RORγt inhibitors.
Wang et al.
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