1,4-DPCA

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1,4-DPCA  纯度: 98.80%

1,4-DPCA,一种有效的选择性脯氨酰-4-羟化酶 (prolyl-4-hydroxylase) 抑制剂,也是人包皮成纤维细胞中的胶原蛋白羟基化抑制剂,IC50 为 2.4 µM。1,4-DPCA 抑制脯氨酰-4-羟化酶 α 同工型,可稳定 HIF-1α 蛋白。1,4-DPCA 还抑制 FIHIC50 为 60 μM。

1,4-DPCA

1,4-DPCA Chemical Structure

CAS No. : 331830-20-7

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1980 In-stock
5 mg ¥1800 In-stock
10 mg ¥3000 In-stock
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100 mg   询价  

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生物活性

1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC50 of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits factor inhibiting HIF (FIH) with an IC50 of 60 μM[1][2].

IC50 & Target

IC50: 2.4 µM (Collagen hydroxylation); 60 μM (Factor inhibiting HIF (FIH))[2]

体外研究
(In Vitro)

1,4-DPCA (24 hours) treatment specifically increases the expression of multiple target genes, including the proangiogenic target genes Vegfa and Hmox1 and proglycolytic targets Ldh-a, Pgk1, Pdk1, and Glut1 in mouse B6 cells[1].
1,4-DPCA treatment significantly reduces the colony sizes of T4-2 (10 μM 1,4-DPCA) and ZR-75-1 cells (20 μM 1,4-DPCA). 1,4-DPCA-treated T4-2 cells form polarized spheroids in 3D culture. 1,4-DPCA treatment significantly reduces invasive branches in DA-MB-157 (20 μM 1,4-DPCA) and MDA-MB-231 (10 μM 1,4-DPCA) cells.1,4-DPCA inhibits the proliferation of T4-2, ZR-75-1, MDA-MB-157 and MDA-MB-231 cells[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

1,4-DPCA treatment suppresses connective tissue ingrowth in porous porous poly (lactic-co-glycolic acid) (PLGA) discs implanted in the peritoneal cavity for 28 days in mice. 1,4-DPCA is found to be effective at inhibiting collagen deposition within and on the outer surface of the disc, and also limited connective tissue ingrowth, but not to the extent of glucocorticoid inhibition[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

240.21

Formula

C13H8N2O3

CAS 号

331830-20-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 12.5 mg/mL (52.04 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.1630 mL 20.8151 mL 41.6302 mL
5 mM 0.8326 mL 4.1630 mL 8.3260 mL
10 mM 0.4163 mL 2.0815 mL 4.1630 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 50% PEG300    50% saline

    Solubility: 10 mg/mL (41.63 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 0.92 mg/mL (3.83 mM); Clear solution

    此方案可获得 ≥ 0.92 mg/mL (3.83 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 9.2 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Yong Zhang, et al. Drug-induced regeneration in adult mice. Sci Transl Med. 2015 Jun 3;7(290):290ra92.

    [2]. Ryan J Love, et al. Transient inhibition of connective tissue infiltration and collagen deposition into porous poly(lactic-co-glycolic acid) discs. J Biomed Mater Res A. 2013 Dec;101(12):3599-606.

    [3]. Gaofeng Xiong, 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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