| 1,4-DPCAcompetitive inhibitor of prolyl 4-hydroxylase |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 98.00%
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| Cas No. | 331830-20-7 | SDF | Download SDF |
| Synonyms | 1,4-dihydrophenonthrolin-4-one-3-Carboxylic acid | ||
| Chemical Name | 4,4α-dihydro-4-oxo-1,10-phenanthroline-3-carboxylic acid | ||
| Canonical SMILES | O=C1C2=C(C3=NC=CC=C3C=C2)N([H])C=C1C(O)=O | ||
| Formula | C13H8N2O3 | M.Wt | 240.2 |
| Solubility | ≤3mg/ml in DMSO;3mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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 shownin 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.
