ISM012-042 is an orally active inhibitor of PHD1 and PHD2, with IC50 values of 1.9 and 2.5 nM, respectively. At a concentration of 2.5 µM, ISM012-042 protects Caco-2 cells from DSS-induced barrier damage. Additionally, in LPS-induced bone marrow-derived dendritic cells (BMDC) from mice, ISM012-042 exhibits anti-inflammatory properties by dose-dependently reducing the expression of IL-12 subunit IL-12p35 and TNF. It also restores intestinal barrier function and alleviates intestinal inflammation in various experimental colitis models. ISM012-042 is useful for studying intestinal mucosal repair and immune disorders.
Molekulargewicht:
488.538
Formel:
C26H28N6O4
Target-Kategorie:
HIF/HIF Prolyl-Hydroxylase
T204762
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