A highly selective

GSK2981278 – 1 mg

Brand:
Cayman
CAS:
1474110-21-8
Storage:
-20
UN-No:
Non-Hazardous - /

GSK2981278 is a highly selective, potent small molecule inhibitor of the retinoic acid receptor-related orphan receptor γ (RORγ). This agent inhibits IL-17A and IL-22 protein secretion from human T cells grown under Th17 skewing conditions in a concentration-dependent manner, with an IC50 value of 3.2 nM.{34217} GSK2981278 also significantly inhibits RORγ transactivation in CHO and Jurkat cells at tested concentrations of 0.1-10 µM.{34217} Topical treatment with GSK2981278 (1% ointment) reduces dermal symptoms in an imiquimod mouse model of psoriasis.{34217} A formulation of this compound is currently in clinical trials to investigate its potential effectiveness against psoriasis.  

 

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Description

A highly selective, potent small molecule inhibitor of RORγ; inhibits RORγ transactivation in cell lines at 0.1-10 µM; inhibits IL-17A and IL-22 secretion from cultured human Th17 cells (IC50 = 3.2 nM)

Formal name: N-(4-ethylphenyl)-3-(hydroxymethyl)-N-(2-methylpropyl)-4-[(tetrahydro-2H-pyran-4-yl)methoxy]-benzenesulfonamide

Synonyms: 

Molecular weight: 461.6

CAS: 1474110-21-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Epigenetics, Transcription, & Translation||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Autoimmunity

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