1,4-DPCA (Synonyms: 1,4-dihydrophenonthrolin-4-one-3-Carboxylic acid) |
Catalog No.GC12845 |
Le 1,4-DPCA, un puissant inhibiteur de la prolyl-4-hydroxylase, est un inhibiteur de l'hydroxylation du collagène dans les fibroblastes du prépuce humain avec une IC50 de 2,4 μM. Le 1,4-DPCA inhibe les isoformes α des prolyl-4-hydroxylases stabilise la protéine HIF-1α. Le 1,4-DPCA inhibe également le facteur inhibiteur du HIF (FIH) avec une IC50 de 60 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 331830-20-7
Sample solution is provided at 25 µL, 10mM.
1,4-DPCA is a competitive inhibitor of prolyl 4-hydroxylase with IC50 value of 3.6 μM [1].
Prolyl hydroxylase catalyzes the formation of hydroxyproline, which has a significant impact on the stability of collagen- the major connective tissue of the human body. Increased collagen deposition produces physical and biochemical signals to sustain tumor growth, resulting in tumor invasion and development. Therefore, 1,4-DPCA has been considered as a treatment strategy to suppress cancer progression as it inhibits collagen synthesis and deposition.
The suppression effect of 1,4-DPCA had been shown in human breast cancer cells. The activity of prolyl-4-hydroxylase was inhibited by 1, 4-DPCA, resulting in decreased deposition of collagen I and IV. In breast tumor cell lines ZR-75-1, T4-2, MDA-MB-157 and MDA-MB-231, treatment with 1,4-DPCA reduced cell proliferation and colony sizes, and formed smaller and less aggressive structures of these four cell lines[2].
References:
[1]. T. J. Franklin, W. P. Morris, P. N. Edwards, et al. Inhibition of prolyl 4-hydroxylase in vitro and in vivo by members of a novel series of phenanthrolinones. Biochemistry Journal 353, 333-338 (2001).
[2]. Xiong G, Deng L, Zhu J, et al. Prolyl-4-hydroxylase α subunit 2 promotes breast cancer progression and metastasis by regulating collagen deposition. BMC Cancer, 2014 Jan 2; 14:1.
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