Cl-Amidine (trifluoroacetate salt)
|Catalog No.: GC11032|
Cl-Amidine (trifluoroacetate salt) 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.
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Sample solution is provided at 25 µL, 10mM.
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TK6 cells are a lymphoblastoid cell line derived from the spleen >30 years ago. HT29 cells are a colon cancer cell line, with mutant p53. TK6 lymphoblastoid cells and HT29 colon cancer cells are cultured with Cl-amidine in a dose-dependent manner (0, 5, 10, 15, 20, 25, 50 μg/mL) over 24 h. Apoptosis is assessed by annexin V/propidium iodide staining followed by flow cytometry.
MiceC57BL/6 mice (8-12 wk old) are fed a standard AIN 93M diet. For this DSS mouse model of colitis, mice receive water ad libitum or 2% DSS beginning at day 0 [for oral gavage/treatment experiment or day 7 [for intraperitoneal/prevention experiment. Initial experiments used injections of Cl-amidine (75 mg/kg-1/day-1 ip), beginning concomitantly with the initiation of 2% DSS in the drinking water. This dose is chosen based on results in a RA model that used 100 mg/kg-1/day-1 without overt side effects and without immunosuppressive outcomes. In DSS model, 50 mice in 4 groups are examined, and inflammation scores are recorded.
. Yuan Luo, et al. Inhibitors and Inactivators of Protein Arginine Deiminase 4: Functional and Structural Characterization. Biochemistry. 2006 Oct 3; 45(39): 11727–11736.
IC50: 5.9 μM
Cl-Amidine is a PAD4 deimination activity inhibitor.
Protein arginine deiminase 4 (PAD4) can catalyze the post-translational modification of arginine residues on histones to form citrulline, which can change gene expression. Thus, dysregulated PAD4 activity has been implicated in cancer and rheumatoid arthritis.
In vitro: Previous study found that Cl-amidine antagonized the PAD4-mediated enhancement of the the p300GBD-GRIP1 interaction dose-dependently, and it was noteworthy that Cl-amidine treatment had only a minimal reduction in the efficiency of the interaction in Cys645S-transfected cells, thereby suggesting that the inhibitory effect of Cl-amidine was not a nonspecific one but was targeted at the active PAD4 enzyme. These results demonstrated that Cl-amidine was significantly more potent than F-amidine, consistent with its improved in vitro potency .
In vivo: Animal study showed that Cl-amidine could improve survival in a mouse model of cecal ligation and puncture (CLP)-induced septic shock. Cl-amidine was proven to play protective roles by restoring innate immune cells in BM, decreasing BM and thymus atrophy, increasing blood monocytes and blood/liver bacteria clearance, and attenuating pro-inflammatory cytokine production in a murine lethal sepsis model .
Clinical trial: So far, no clinical study has been conducted.
 Luo, Y. ,Arita, K.,Bhatia, M., et al. Inhibitors and inactivators of protein arginine deiminase 4: Functional and structural characterization. Biochemistry 45(39), 11727-11736 (2006).
 Zhao T, Pan B, Alam HB, Liu B, Bronson RT, Deng Q, Wu E, Li Y. Protective effect of Cl-amidine against CLP-induced lethal septic shock in mice. Sci Rep. 2016 Nov 7;6:36696.
|Chemical Name||N-[(1S)-1-(aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-benzamide 2,2,2-trifluoroacetate|
|Formula||C14H19ClN4O2 • CF3CO2H||M.Wt||424.8|
|Solubility||DMF: 14 mg/ml, DMSO: 100 mg/ml, water: 3 mg/ml||Storage||Store at -20°C|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
|Shipping Condition||Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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