Drug intelligence / Profile preview

dimethyloxalylglycine

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral, Subcutaneous
01

Overview

Dimethyloxalylglycine is a cell-permeable synthetic **small molecule** that functions as a competitive inhibitor of prolyl-4-hydroxylase domain (PHD) enzymes and factor inhibiting HIF (FIH), both of which regulate the stability and transcriptional activity of hypoxia-inducible factor (HIF) proteins[1][2][3][5][7][8]. Inhibition of PHDs by DMOG leads to HIF stabilization and activation, stimulating pro-angiogenic pathways (notably via upregulation of VEGF and eNOS) and showing **neuroprotective** and anti-ischemic effects in animal models[1][3][5]. DMOG also inhibits hepatic lipogenesis by suppression of SREBP1c, apparently via both canonical (HIF/INSIG2-dependent) and non-canonical pathways[7]. It is used primarily as a **research tool** and is not approved for clinical use in humans.

Other names
N-(methoxyoxoacetyl)-glycine methyl estermethyl 2-(2-methoxy-2-oxoacetamido)acetateN-oxalylglycine dimethyl ester
02

Targets

FIH-1 (Factor inhibiting hypoxia-inducible factor 1)EGLN1 (Prolyl hydroxylase domain-containing protein 2)PHD3 (Prolyl hydroxylase domain-containing protein 3)PHD1 (Prolyl hydroxylase domain-containing protein 1)

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