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GSK 2981278

Chemical Structure : GSK 2981278

CAS No.: 1474110-21-8

GSK 2981278 (GSK2981278;GSK-2981278)

Catalog No.: PC-60455Not For Human Use, Lab Use Only.

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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.
GSK 2981278 shows no effects on RORα-dependent activation.
GSK 2981278 robustly inhibits RORγ-mediated cytokine production at both the mRNA and protein level, inhibits RORγt-mediated transactivation; attenuates inflammation in mouse model of psoriasis.

Physicochemical Properties

M.Wt 461.617
Formula C25H35NO5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(4-Ethylphenyl)-3-(hydroxymethyl)-N-(2-methylpropyl)-4-[(tetrahydro-2H-pyran-4-yl)methoxy]benzenesulfonamide

References

1. Kang EG, et al. Br J Dermatol. 2017 Nov 18. doi: 10.1111/bjd.16131.

2. Smith SH, et al. PLoS One. 2016 Feb 12;11(2):e0147979.

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