| Identification | Back Directory | [Name]
Cl-Amidine | [CAS]
913723-61-2 | [Synonyms]
Cl-Amidine
N-alpha-Benzoyl-N5-(2-chloro-1-iminoethyl)-1-ornithine amide
N-[(1S)-1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]benzamide
Benzamide, N-[(1S)-1-(aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-
N-[(1S)-1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-benzamideN- | [Molecular Formula]
C14H19ClN4O2 | [MDL Number]
MFCD20278255 | [MOL File]
913723-61-2.mol | [Molecular Weight]
310.78 |
| Hazard Information | Back Directory | [Uses]
Cl-amidine is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine induces apoptosis in cancer cells. Cl-amidine induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model[1][2][3][4][5]. | [Definition]
ChEBI: Cl-Amidine is a member of benzenes. | [Biological Activity]
Cl-amidine is an orally active PAD inhibitor with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3 and PAD4, respectively.It induces apoptosis in cancer cells. And Cl-Amidine blocks histone 3 citrullination and neutrophil extracellular trap formation and improves survival in mice with sepsis. | [in vivo]
Cl-amidine (75 mg/kg, ip once daily) suppresses and treats DSS-induced colitis in mice[2].
Cl-amidine (5, 25, 75 mg/kg, oral gavage, once daily) leads to significant reductions in the histology scores dose-dependently[2]. | Animal Model: | C57BL/6 mice (8-12 wk old, DSS mouse model of colitis)[2]. | | Dosage: | 75 mg/kg. | | Administration: | IP once daily. | | Result: | Suppressed PAD activity, protein citrullination, and PAD levels in the colon in vivo. |
| Animal Model: | C57BL/6 mice (8-12 wk old, DSS mouse model of colitis)[2]. | | Dosage: | 5, 25, 75 mg/kg. | | Administration: | Oral gavage once daily. | | Result: | Led to significant reductions in the histology scores. |
| [target]
IC50: 0.8 μM (PAD1), 5.9 μM (PAD4), 6.2 μM (PAD3). | [References]
[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. DOI:10.1021/bi061180d
[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. DOI:10.1152/ajpgi.00435.2010
[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. DOI:10.18632/oncotarget.5937
[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. DOI:10.1159/000448808
[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. DOI:10.1021/bi100363t |
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InvivoChem
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13549236410 |
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https://www.invivochem.cn/ |
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