GSK2981278 is a highly potent and selective inverse agonist for RORγ.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
AGONIST
Mechanism of action
Agonist of RAR-related orphan receptor-γ
Product Description
Information
GSK2981278 GSK2981278 is a highly potent and selective inverse agonist for RORγ .
Targets
RORγ
In vitro
GSK2981278 has no significant effect on RORα-dependent activation. GSK2981278 significantly inhibits production of the Th17 signature (IL-17A, IL-17F, IL-22 and IL-23) in multiple in vitro and human tissue-based assays.
In vivo
GSK2981278 attenuates inflammation in a mouse model of psoriasis. Topical treatment with GSK2981278 will significantly limit Th17-type cytokine expression and should therefore lead to improved clinical outcomes for patients.
1.Skepner J, Ramesh R, Trocha M, Schmidt D, Baloglu E, Lobera M, Carlson T, Hill J, Orband-Miller LA, Barnes A et al.. (2014) Pharmacologic inhibition of RORγt regulates Th17 signature gene expression and suppresses cutaneous inflammation in vivo.. J Immunol, 192 (6):(2564-75). [PMID:24516202][10.1021/op500134e]
2.Smith SH, Peredo CE, Takeda Y, Bui T, Neil J, Rickard D, Millerman E, Therrien JP, Nicodeme E, Brusq JM et al.. (2016) Development of a Topical Treatment for Psoriasis Targeting RORγ: From Bench to Skin.. PLoS ONE, 11 (2):(e0147979). [PMID:26870941][10.1021/op500134e]
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G2227601