1,4-DPCA

An inhibitor of prolyl 4-hydroxylase

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库存: 现货

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5mg

￥800.00

640.00

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10mg

￥1425.00

1140.00

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25mg

￥3150.00

2520.00

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50mg

￥5450.00

4360.00

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货号: ajci9932
CAS: 331830-20-7
别名: 1,4-dihydrophenonthrolin-4-one-3-Carboxylic acid
分子式: C13H8N2O3
分子量: 240.2
纯度: >98%
溶解度: ≤3mg/ml in DMSO;3mg/ml in dimethyl formamide
储存: Store at -20°C
库存: 现货

Background

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].

参考文献:
[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.