Chemical Name: 8-Methoxy-6-[7-(2-morpholin-4-ylethoxy)imidazo[1,2-a]pyridin-3-yl]-2-(2,2,2-trifluoroethyl)-3,4-dihydroisoquinolin-1-one
SIK2/3 inhibitor
Molekulargewicht:
504.51
Reinheit:
>98% by HPLC NMR (conforms)
Formulierung:
Off-white solid
CAS Nummer:
[2403733-82-2]
Formel:
C25H27F3N4O4
Anwendungsbeschreibung:
GLPG3970 is a potent and selective (against a panel of 372 kinases) SIK2/3 inhibitor (IC50s: SIK2 = 7.8 nM, SIK3 = 3.8 nM).1 It reduced THFalpha and increased IL-10 levels in an LPS challenge model in mice and displayed efficacy in a mouse model of colitis. GLPG3970 promoted reprogramming of human myeloid cells toward an anti-inflammatory phenotype, reprogrammed monocyte-dendritic differentiation toward stable tolerogenic phenotypes, and suppressed T-cell activation.2 It also displayed efficacy in mouse models of psoriasis and arthritis.
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