Biological Activity:

1,4-DPCA is a selective and cell permeable prolyl 4-hydroxylase (P4H) inhibitor. It inhibits α-prolyl 4-hydroxylase, an oxygen-sensing enzyme that targets the pro-angiogenic factor HIF-1α for destruction upon hydroxylation of a specific proline residue. It also inhibits asparaginyl-hydroxylase factor inhibiting HIF (FIH) and is useful for controlling excess collagen deposition in pathological fibrosis.

How to Use:

In vitro: 1,4-DPCA was used at 10 µM final concentration in vitro and in cellular assays.
In vivo: n/a

Reference:

• 1. Jaakkola P, et al. Targeting of HIF-alpha to the von Hippel-Lindau ubiquitylation complex by O2-regulated prolyl hydroxylation. (2001) Science. 292(5516):468-72. 
• 2. Franklin TJ, et al. Inhibition of prolyl 4-hydroxylase in vitro and in vivo by members of a novel series of phenanthrolinones. (2001) Biochem J. 353(Pt 2):333-8.
• 3. Banerji B, et al. The inhibition of factor inhibiting hypoxia-inducible factor (FIH) by beta-oxocarboxylic acids. (2005) Chem Commun (Camb). (43):5438-40.