详情描述
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.
Products are for research use only. Not for human use.