Cl-amidine |
カタログ番号GC35706 |
Cl-アミジンは、PAD1、PAD3、PAD4 の IC50 値がそれぞれ 0.8 μM、6.2 μM、5.9 μM の経口活性ペプチジルアルギニン デミナーゼ (PAD) 阻害剤です。
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Cas No.: 913723-61-2
Sample solution is provided at 25 µL, 10mM.
Cl-amidine (N-α-benzoyl-N5-(2-chloro-1-iminoethyl)-l-ornithine amide), is a PAD4 inactivator with enhanced potency. PAD Inhibitor was proved to exhibit enhanced cell killing in PAD-expressing osteosarcoma cells and block the formation of neutrophil extracellular traps. Cl-amidine, as a PAD inhibitor, could reduce the clinical signs and symptoms of colitis, and induced apoptosis of inflammatory cells. The inhibition of PAD by Cl-amidine markedly suppresses the production of CitH3, and neutralization of CitH3 improves survival markedly in septic mice.[1][2]
Cl-amidine is a more potent inhibitor of PAD which has the IC50 of 5.9 ± 0.3 μM. In vitro experiment indicated that Cl-amidine caused a cell cycle arrest at the G1 phase and miRNA-16 induction through a p53-mediated mechanism. In vivo experiment demonstrated that the enhancement of the p300GBD–GRIP1 interaction mediated by PAD4 was antagonized by Cl-amidine in a dose-dependent manner, and that Cl-amidine treatment caused only a minimal reduction in the efficiency of the interaction, indicating that the inhibitory effect of this compound targeted at the active PAD4 enzyme.[1][3]
References:
[1]. Luo Y, et al. Inhibitors and inactivators of protein arginine deiminase 4: functional and structural characterization. Biochemistry. 2006 Oct 3;45(39):11727-36.
[2].Ting Z, et al. Protective effect of Cl-amidine against CLP-induced lethal septic shock in mice. Sci Rep. 2016; 6: 36696
[3].Cui X, et al. The induction of microRNA-16 in colon cancer cells by protein arginine deiminase inhibition causes a p53-dependent cell cycle arrest. PLoS One. 2013;8(1):e53791.
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