Cl-amidine is a peptidylarginine deminase (PAD) inhibitor, with an IC50 5.9±0.3 μM for PAD4.
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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]. |
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存储液制备 | ![]() |
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 |
CAS号 | 1043444-18-3 |
分子式 | C16H20ClF3N4O4 |
分子量 | 424.8 |
SMILES Code | O=C(N)[C@@H](NC(C1=CC=CC=C1)=O)CCCNC(CCl)=N.O=C(O)C(F)(F)F |
MDL No. | MFCD31536783 |
别名 | Cl-amidine |
运输 | 蓝冰 |
InChI Key | WUSNMVYWOLUWDD-MERQFXBCSA-N |
Pubchem ID | 57402549 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, inert atmosphere, 2-8°C |