GSK 2981278

GSK 2981278 (GSK2981278) is a potent, highly selective RORγ/RORγt inhibitor that potently inhibits IL-17A and IL-22 protein secretion in human peripheral T cell with IC50 of 3.2 nM; shows no effects on RORα-dependent activation; robustly inhibits RORγ-mediated cytokine production at both the mRNA and protein level, inhibits RORγt-mediated transactivation; attenuates inflammation in mouse model of psoriasis.Psoriasis Phase 2 Clinical (In Vitro) :GSK2981278 markedly and potently inhibits IL-17A and IL-22 protein secretion in a concentration dependent manner (IC50 = 3.2 nM) during 5 days of culture under Th17 skewing conditions.GSK2981278 (0.3, 1, 3, 10, 30, 100, 300, 1000 pM; 5 day) potently and selectively inhibits IL-17 and IL-22 levels. Culture in the presence of ≥3 nM GSK2981278 led to a near-complete inhibition of IL-17A protein secretion. (In Vivo) :GSK2981278 (1% in ointment; topically; for three days) reduces skin redness and scaling, as well as decreased hyperplasia, as evidenced by a 23% reduction in epidermal thickness. GSK2981278 attenuates inflammation in a mouse model of psoriasis.

1474110-21-8

GSK2981278 | GSK-2981278

>98% (HPLC)

DMSO: 10 mM (< 1 mg/ml refers to the product slightly soluble or insoluble)

O=S (C1=CC=C (OCC2CCOCC2) C (CO) =C1) (N (C3=CC=C (CC) C=C3) CC (C) C) =O

C25H35NO5S

461.617

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.