2,4-Pyridinedicarboxylic Acid
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
2,4-吡啶二羧酸(2,4-PDCA)是一种组蛋白赖氨酸特异性去甲基化酶抑制剂,其靶向JMJD2A(KDM4A)\KDM4C\KDM4E(IC50为1.4 μM)\KDM5B(IC50为3 μM)\KDM6A以及其他2-加氧酶[1][2].
组蛋白赖氨酸特异性去甲基化酶JMJD2A(KDM4A)和KDM4C都是Jumonji结构域2(JMJD2)家族的成员,作为三甲基化特异性去甲基化酶,将特定三甲基化组蛋白残基转化为二甲基化形式.KDM5B是一种H3K4me3/ ME2特异性赖氨酸去甲基化酶[1][2].
2,4-吡啶二羧酸(2,4-PDCA)是一种JMJD2 A(KDM4A)\KDM4C和KDM5B抑制剂.在FDH偶联实验中,2,4-PDCA抑制ccKDM5B,IC50值为3±1 μM.在H3(1-21)K4me3的MALDI-TOF分析中,2,4-PDCA减少ccKDM5B诱导的H3(1-15)水平.在转染 KDM5B的U2-OS细胞中,2,4-PDCA抑制H3K4me3的下降[1].接受HG处理的血管平滑肌细胞(VSMCs)中,2,4-PDCA(1.0 mM)浓度依赖性地抑制JMJD2A和HG诱导的增殖,并抑制HG诱导的迁移.2,4-PDCA还减少MCP-1和IL-6的mRNA和蛋白水平[2].
在糖尿病大鼠中,2,4-PDCA(7.5 mg/kg/d)可减少损伤28天后受损血管中的新内膜面积以及I/M比.2,4-PDCA也抑制新内膜中PCNA阳性细胞的百分比[2].
参考文献：
[1]. Kristensen LH, Nielsen AL, Helgstrand C, et al. Studies of H3K4me3 demethylation by KDM5B/Jarid1B/PLU1 reveals strong substrate recognition in vitro and identifies 2,4-pyridine-dicarboxylic acid as an in vitro and in cell inhibitor. FEBS J, 2012, 279(11): 1905-1914.
[2]. Qi H, Jing Z, Xiaolin W, et al. Histone Demethylase JMJD2A Inhibition Attenuates Neointimal Hyperplasia in the Carotid Arteries of Balloon-Injured Diabetic Rats via Transcriptional Silencing: Inflammatory Gene Expression in Vascular Smooth Muscle Cells. Cell Physiol Biochem, 2015, 37(2): 719-734.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 167.12 |
| Cas No. | 499-80-9 |
| Formula | C7H5NO4 |
| Solubility | insoluble in H2O; ≥11.2 mg/mL in EtOH with ultrasonic; ≥9.15 mg/mL in DMSO |
| Chemical Name | pyridine-2,4-dicarboxylic acid |
| SDF | Download SDF |
| Canonical SMILES | O=C(O)C1=CC(C(O)=O)=NC=C1 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
质量控制和MSDS
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化学结构
