產(chǎn)品說明
脯氨酰4-羥化酶的競(jìng)爭(zhēng)性抑制劑
該產(chǎn)品包含在以下化合物庫(kù)中:
質(zhì)量控制
化學(xué)性質(zhì)
| CAS號(hào) | 331830-20-7 | ? | ? |
| 別名 | 1,4-dihydrophenonthrolin-4-one-3-Carboxylic acid |
| 分子式 | C13H8N2O3 | 分子量 | 240.2 |
| 溶解性 | Soluble in DMSO | 儲(chǔ)存條件 | Store at -20° |
?
實(shí)驗(yàn)操作
| 細(xì)胞實(shí)驗(yàn)[2]： |
| 細(xì)胞系 | |
| 溶解方法 | |
| 反應(yīng)時(shí)間 | |
| 應(yīng)用 | |
| 動(dòng)物實(shí)驗(yàn)[3]： |
| 動(dòng)物模型 | |
| 劑量 | |
| 注意事項(xiàng) | |
| References: |
產(chǎn)品描述
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.
溫馨提示：不可用于臨床治療。