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1,4-DPCA {[allProObj[0].p_purity_real_show]}

货号:A1340294 同义名: 1,4-dihydrophenonthrolin-4-one-3-Carboxylic acid Ambeed 开学季,买赠积分,赢豪礼

1,4-DPCA是一种有效的脯氨酰-4-羟化酶抑制剂,IC50 为 2.4 μM,能够抑制 HIF-1α 的降解,从而稳定 HIF-1α 蛋白,同时抑制 FIH,IC50 为 60 μM,适用于缺氧相关疾病及纤维化的研究。

1,4-DPCA 化学结构 CAS号:331830-20-7
1,4-DPCA 化学结构
CAS号:331830-20-7
1,4-DPCA 3D分子结构
CAS号:331830-20-7
1,4-DPCA 化学结构 CAS号:331830-20-7
1,4-DPCA 3D分子结构 CAS号:331830-20-7
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1,4-DPCA 纯度/质量文件 产品仅供科研

货号:A1340294 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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产品名称 HIF HIF1 PHD1 PHD2 PHD3 其他靶点 纯度
KC7F2 +

HIF-1α, IC50: 20 μM

+

HIF-1α, IC50: 20 μM

{[allProObj[0].p_purity_real_show]}
Lificiguat {[allProObj[0].p_purity_real_show]}
BAY 87-2243 {[allProObj[0].p_purity_real_show]}
PX-478·2HCl {[allProObj[0].p_purity_real_show]}
2-Methoxyestradiol {[allProObj[0].p_purity_real_show]}
CAY10585 ++

HIF, IC50: 4.4 μM

BCRP {[allProObj[0].p_purity_real_show]}
DMOG {[allProObj[0].p_purity_real_show]}
FG 2216 ++

PHD2, IC50: 3.9 μM

{[allProObj[0].p_purity_real_show]}
MK-8617 ++++

PHD1, IC50: 1 nM

++++

PHD2, IC50: 1 nM

++++

PHD3, IC50: 14 nM

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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

1,4-DPCA 生物活性

描述 1,4-DPCA is a potent inhibitor of prolyl-4-hydroxylase with an IC50 of 2.4 µM in human foreskin fibroblasts. 1,4-DPCA can inhibit the α isoenzyme of prolyl-4-hydroxylase and stabilize HIF-1α protein. 1,4-DPCA also inhibits factors that inhibit HIF with an IC50 of 60 µM[1][2].In mouse B6 cells, 1,4-DPCA specifically increases the expression of several target genes, including the pro-angiogenic targets Vegfa and Hmox1, and the proglycolytic targets Ldh-a, Pgk1, Pdk1, and Glut1, after 24 hours of treatment[1].1,4-DPCA significantly reduced cell colony size in T4-2 (10 μM) and ZR-75-1 cells (20 μM). T4-2 cells treated with 1,4-DPCA formed polarised spheroids in three-dimensional cultures. 1,4-DPCA treatment significantly reduced invasive branching in DA-MB-157 (20 μM) and MDA-MB-231 (10 μM) cells[3].

1,4-DPCA 动物研究

Animal study 1,4-DPCA inhibited the growth of connective tissue resulting from PLGA discs implanted in the abdominal cavity of mice 28 days after implantation. It was found that 1,4-DPCA was effective in inhibiting collagen deposition on the internal and external surfaces of the discs, as well as limiting connective tissue growth, but not to the same extent as glucocorticoids[2].

1,4-DPCA 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.

1,4-DPCA 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.16mL

0.83mL

0.42mL

20.81mL

4.16mL

2.08mL

41.63mL

8.33mL

4.16mL

1,4-DPCA 技术信息

CAS号331830-20-7
分子式C13H8N2O3
分子量 240.214
别名 1,4-dihydrophenonthrolin-4-one-3-Carboxylic acid
运输蓝冰
存储条件

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 12 mg/mL(49.96 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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