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IC50: 9.3 and 3.7 μM for hydroxyproline synthesis inhibition of embryonic chicken lung extracted from tissue and culture medium [1].

Dimethyloxalylglycine (DMOG) is an inhibitor of prolyl-4-hydroxylase domain (PHD) enzymes that regulate the stability of hypoxia-inducible factor (HIF). Localized tissue hypoxia is a feature of infection and inflammation, leading to the upregulation of the transcription factors HIF-1α and NF-κB via inhibition of oxygen sensing hydroxylase enzymes.

In vitro: DMOG acts to stabilize HIF-1a expression under normal oxygen tension in cultured cells at concentrations from 0.1 to 1 mmol/L [2].

In vivo: Pre-treatment with DMOG attenuates systemic LPS-induced activation of the NF-κB pathway. Furthermore, mice treated with DMOG had significantly increased survival in LPS-induced shock. In addition, in vivo DMOG treatment upregulates the expression of IL-10, specifically in the peritoneal B-1 cell population [3].

Clinical trial: Currently no clinical data are available.

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