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F-Amidine (trifluoroacetate salt) Sale

目录号 : GC43651

A PAD inhibitor

F-Amidine (trifluoroacetate salt) Chemical Structure

Cas No.:877617-46-4

规格 价格 库存 购买数量
100μg
¥428.00
现货
250μg
¥1,010.00
现货
500μg
¥1,936.00
现货
1mg
¥3,426.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

F-amidine is an inhibitor of protein arginine deiminases (PADs) that is selective for PAD1 and PAD4 (IC50s = 29.5, 350, and 21.6 µM for PAD1, PAD3, and PAD4 in vitro, respectively). It irreversibly inactivates all four PAD subtypes (kinact/KI = 2,800, 380, 170, and 3,000 M-1min-1 by covalently modifying an active site cysteine that is important for its catalytic activity. F-amidine is cytotoxic to HL-60, MCF-7, and HT-29 cancer cell lines (IC50s = 0.5, 0.5 and 1 μM, respectively).

Chemical Properties

Cas No. 877617-46-4 SDF
Canonical SMILES FC(F)(C(O)=O)F.NC([C@@H](NC(C1=CC=CC=C1)=O)CCCNC(CF)=N)=O
分子式 C14H19FN4O2•CF3COOH 分子量 408.4
溶解度 DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 10 mg/ml 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.4486 mL 12.2429 mL 24.4858 mL
5 mM 0.4897 mL 2.4486 mL 4.8972 mL
10 mM 0.2449 mL 1.2243 mL 2.4486 mL
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Research Update

CXCL1-Triggered PAD4 Cytoplasmic Translocation Enhances Neutrophil Adhesion through Citrullination of PDIA1

J Atheroscler Thromb 2022 Sep 1;29(9):1307-1318.PMID:34880166DOI:PMC9444809

Aims: Vascular inflammation is critical for the development and progression of atherosclerosis. Previously, we reported that neutrophils adhere to the vascular endothelium in low-density lipoprotein receptor null mice fed a high-fat diet through hypercitrullination of histone H3 by peptidylarginine deiminase 4 (PAD4) in neutrophils. However, the involvement of PAD4 and citrullination of proteins other than histone H3 in neutrophil adhesion is not well known. In this study, we investigated the function of PAD4 and identified citrullinated proteins during vascular inflammation. Methods: We pefformed flow assay under physiological flow conditions using differentiated HL-60 (dHL-60) cells stimulated with CXCL1 and human umbilical vein endothelial cells (HUVECs). Furthermore, phalloidin stain for dHL-60 stimulated with CXCL1 to observe F-actin polymerization and immunohistochemistry for the activated β2-integrin was conducted. To identify a target of citrullination in the cytoplasm of dHL-60 cells, liquid chromatography-mass spectrometry (LC-MS/MS) for dHL-60 stimulated with CXCL1 was performed. Results: Inhibition or knockdown of PAD4 significantly decreased adhesion of under physiological flow conditions. Thr-Asp-F-amidine trifluoroacetate salt (TDFA), a PAD4 inhibitor, inhibited cytoplasmic translocation of PAD4 by CXCL1. TDFA or knockdown of PAD4 significantly decreased expression of β2-integrin and F-actin polymerization activated by CXCL1. Moreover, LC-MS/MS identified protein disulfide isomerase A1 (PDIA1) as a target of citrullination in the cytoplasm of dHL-60 cells. Knockdown of PDIA1 significantly decreased adhesion of dHL-60 cells to HUVECs, expression of β2-integrin, and F-actin polymerization. Conclusions: Cytoplasmic translocation of PAD4 by CXCL1 induces neutrophil adhesion to vascular endothelial cells and citrullination of PDIA1.