1,4-DPCA
(Synonyms: 1,4-dihydrophenonthrolin-4-one-3-Carboxylic acid) 目录号 : GC128451,4-DPCA一种有效的选择性脯氨酰-4-羟化酶抑制剂（IC50=2.4μM），也可抑制天冬酰胺羟化酶因子FIH活性（IC50=60μM）。
Cas No.:331830-20-7
Sample solution is provided at 25 µL, 10mM.
1,4-DPCA is a potent and selective prolyl-4-hydroxylase inhibitor (IC₅₀=2.4μM) that also suppresses the activity of asparagine hydroxylase factor FIH (IC₅₀=60μM)[1-2]. 1,4-DPCA has potential applications in the treatment of myocardial infarction[3-4].
In vitro, treatment of various breast cancer cell lines (including T4-2, ZR-75-1, MDA-MB-157, and MDA-MB-231) cultured in three-dimensional models with 1,4-DPCA (10–20μM) for 4 days significantly inhibited cell proliferation and reduced invasive phenotypes[5]. Exposure of multiple cell lines (such as H9C2, L929, and cardiomyocytes) to 1,4-DPCA (10–20μM) markedly upregulated HIF-1α protein expression and enhanced cell proliferation [6].
In vivo, a single intramyocardial injection of 1,4-DPCA (delivered via ALG-CHO-TA/DPCA@PDA/MMP-SP/HA-SH hydrogel) at a dose of 100μL (equivalent to 0.4mg/kg) in a rat model of myocardial infarction significantly improved cardiac function and promoted myocardial repair[7]. In a lipopolysaccharide (LPS)-induced septic acute lung injury model in 6–8 week-old C57BL/6J mice, a single tail vein injection of 1,4-DPCA (10mg/kg) acted as a HIF-1α activator, effectively reversing the protective effect of GDF15 overexpression against lung injury[8].
References:
[1] Zhang Y, Strehin I, Bedelbaeva K, et al. Drug-induced regeneration in adult mice. Sci Transl Med. 2015 Jun 3;7(290):290ra92.
[2] Love RJ, Jones KS. 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] Wang K, Yao SY, Wang Z, et al. A Sequential Dual Functional Supramolecular Hydrogel with Promoted Drug Release to Scavenge ROS and Stabilize HIF-1α for Myocardial Infarction Treatment. Adv Healthc Mater. 2024 Mar;13(6):e2302940.
[4] Zebrowitz E, Aslanukov A, Kajikawa T, et al. Prolyl-hydroxylase inhibitor-induced regeneration of alveolar bone and soft tissue in a mouse model of periodontitis through metabolic reprogramming. Front Dent Med. 2022;3:992722.
[5] 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.
[6] Deng K, Hua Y, Gao Y, et al. Thermosensitive Hydrogel with Programmable, Self-Regulated HIF-1α Stabilizer Release for Myocardial Infarction Treatment. Adv Sci (Weinh). 2024 Nov;11(43):e2408013.
[7] Wei X, Chen S, Xie T, et al. An MMP-degradable and conductive hydrogel to stabilize HIF-1α for recovering cardiac functions. Theranostics. 2022 Jan 1;12(1):127-142.
[8] Kuang X, Niu Z, Huang Z, et al. GDF15 attenuates sepsis-induced acute lung injury by suppressing the HIF-1α/LDHA pathway. Int Immunopharmacol. 2025 Oct 10;163:115198.
1,4-DPCA一种有效的选择性脯氨酰-4-羟化酶抑制剂（IC50=2.4μM），也可抑制天冬酰胺羟化酶因子FIH活性（IC50=60μM）[1-2]。1,4-DPCA可用心肌梗死治疗[3-4]。
在体外，1,4-DPCA（10–20μM）处理多种乳腺癌细胞系（包括T4-2、ZR-75-1、MDA-MB-157和MDA-MB-231）的三维培养模型4天，显著抑制了细胞增殖并减弱了侵袭性表型[5]。1,4-DPCA（10–20μM）处理多种细胞系（包括H9C2、L929细胞及心肌细胞），显著上调了HIF-1α蛋白的表达水平并促进了细胞增殖[6]。
在体内，1,4-DPCA水凝胶在心肌梗死模型大鼠中进行单次心肌内注射（100μL；0.4mg/kg）。1,4-DPCA显著改善了心脏功能并促进了心肌修复 [7]。1,4-DPCA（10mg/kg）通过尾静脉单次注射，用于处理6-8周龄C57BL/6J小鼠的LPS诱导的脓毒症急性肺损伤模型。1,4-DPCA作为HIF-1α激活剂，显著逆转了GDF15过表达对肺损伤的保护作用[8]。
| Cell experiment [1]: | |
Cell lines | HMT-3522 T4-2, MDA-MB-231, ZR-75-1, and MDA-MB-157 breast cancer cell lines |
Preparation Method | Cells were cultured in three-dimensional (3D) laminin-rich extracellular matrix (lrECM) on-top cultures. T4-2 and ZR-75-1 cells were seeded at a density of 2.1×10⁴ cells per cm²; MDA-MB-157 and MDA-MB-231 cells were seeded at 1.4×10⁴ cells per cm². Cells were treated with 1,4-DPCA (10–20μM) at specified concentrations for 4 days. |
Reaction Conditions | 10–20μM; 4 days |
Applications | 1,4-DPCA significantly reduced colony sizes of T4-2 and ZR-75-1 cells and suppressed invasive branches in MDA-MB-231 and MDA-MB-157 cells in 3D culture. Treatment with 1,4-DPCA also inhibited cell proliferation, as evidenced by decreased EdU-positive cells, and impaired collagen I and IV deposition. |
| Animal experiment [2]: | |
Animal models | C57BL/6J mice |
Preparation Method | Mice were intravenously injected with rAAV8-CMV-mGdf15 or control vector(rAAV8-CMV-LacZ). After 1 week of viral expression, acute lung injury(ALI) was induced by intraperitoneal injection of LPS (20mg/kg). 1,4-DPCA (10mg/kg) was administered via tail vein injection 2 hours prior to LPS challenge. |
Dosage form | 10mg/kg; i.v; Single injection. |
Applications | 1,4-DPCA administration partially abolished the protective effects of GDF15 overexpression on LPS-induced lung injury, as evidenced by increased expression of endothelial adhesion molecules (VCAM-1 and ICAM-1) and elevated serum pro-inflammatory cytokine levels (IL-6 and TNF-α). 1,4-DPCA also reversed GDF15-mediated suppression of HIF-1α/LDHA pathway activation. |
References: | |
| Cas No. | 331830-20-7 | SDF | |
| 别名 | 1,4-dihydrophenonthrolin-4-one-3-Carboxylic acid | ||
| 化学名 | 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 | ||
| 分子式 | C13H8N2O3 | 分子量 | 240.2 |
| 溶解度 | ≤3mg/ml in DMSO;3mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.1632 mL | 20.816 mL | 41.632 mL |
| 5 mM | 832.6 μL | 4.1632 mL | 8.3264 mL |
| 10 mM | 416.3 μL | 2.0816 mL | 4.1632 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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