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Cl-amidine TFA

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Chemical Structure| 1043444-18-3 同义名 : Cl-amidine
CAS号 : 1043444-18-3
货号 : A1209276
分子式 : C16H20ClF3N4O4
纯度 : 99%+
分子量 : 424.803
MDL号 : MFCD31536783
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 Cl-amidine TFA, an ingestible inhibitor of peptidylarginine deminase (PAD), exhibits IC50 values of 0.8 μM for PAD1, 6.2 μM for PAD3, and 5.9 μM for PAD4. It prompts apoptosis in cancerous cells and stimulates the expression of microRNA-16, leading to cell cycle arrest. Additionally, Cl-amidine TFA blocks the citrullination of histone 3 and the formation of neutrophil extracellular traps, thereby enhancing survival rates in a mouse model of sepsis[1][2][3][4][5]. Cl-amidine, at varying concentrations (0, 5, 10, 15, 20, 25, 50 μg/mL) over a 24-hour period, triggers cell death through apoptosis in TK6 lymphoblastoid cells and HT29 colon cancer cells, with the effect intensifying with higher doses. Notably, HT29 cells exhibit a comparative resistance to the apoptotic effects induced by Cl-amidine[2]. Cl-amidine permanently deactivates PAD enzymes through the covalent alteration of a crucial cysteine residue within the active site, which is essential for the enzyme's catalytic function[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.35mL

0.47mL

0.24mL

11.77mL

2.35mL

1.18mL

23.54mL

4.71mL

2.35mL
参考文献

[1]Yuan Luo, et al. Inhibitors and Inactivators of Protein Arginine Deiminase 4: Functional and Structural Characterization. Biochemistry. 2006 Oct 3; 45(39): 11727–11736.

[2]Chumanevich AA, et al. Suppression of colitis in mice by Cl-amidine: a novel peptidylarginine deiminase inhibitor. Am J Physiol Gastrointest Liver Physiol. 2011 Jun;300(6):G929-38.

[3]Witalison EE, et al. Molecular targeting of protein arginine deiminases to suppress colitis and prevent colon cancer. Oncotarget. 2015 Nov 3;6(34):36053-62.

[4]Biron BM, et al., Cl-Amidine Prevents Histone 3 Citrullination and Neutrophil Extracellular Trap Formation, and Improves Survival in a Murine Sepsis Model. J Innate Immun. 2017;9(1):22-32.

[5]Bryan Knuckley, et al. Substrate Specificity and Kinetic Studies of PADs 1, 3, and 4 Identify Potent and Selective Inhibitors of Protein Arginine Deiminase 3. Biochemistry. 2010 Jun 15;49(23):4852-63.