diethyl-pyimdc

Description: Diethyl pyimDC is a novel inhibitor of human CP4H1 (collagen prolyl 4-hydroxylase 1). Collagen is the most abundant protein in animals. Its overproduction is associated with fibrosis and cancer metastasis. The stability of collagen relies on post-translational modifications, the most prevalent being the hydroxylation of collagen strands by collagen prolyl 4-hydroxylases (CP4Hs). Catalysis by CP4Hs enlists an iron cofactor to convert proline residues to 4-hydroxyproline residues, which are essential for the conformational stability of mature collagen. Ethyl 3, 4-dihydroxybenzoate (EDHB) is commonly used as a 'P4H' inhibitor in cells, but suffers from low potency, poor selectivity, and off-target effects that cause iron deficiency.

References: ACS Chem Biol. 2016 Jan 15; 11(1):193-9.