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Cl-amidine TFA

Chemical Structure : Cl-amidine TFA

CAS No.: 1043444-18-3

Cl-amidine TFA (pan-PAD inhibitor)

Catalog No.: PC-22866Not For Human Use, Lab Use Only.

Cl-amidine TFA is a potent, irreversible, orall active inhibitor of protein arginine deiminases (PADs) with IC50 of 0.8, 6.2, and 5.9 µM for PAD1, PAD3, and PAD4, respectively.

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Biological Activity

Cl-amidine TFA is a potent, irreversible, orall active inhibitor of protein arginine deiminases (PADs) with IC50 of 0.8, 6.2, and 5.9 µM for PAD1, PAD3, and PAD4, respectively.
Cl-amidine is cytotoxic to HL-60, MCF-7, and HT-29 cancer cells (IC50s = 0.25, 0.05, and 1 μM, respectively).
Cl-amidine (50 mg/kg) reduces ex vivo extracellular neutrophil extracellular trap (NET) formation and increases survival in a mouse model of sepsis induced by cecal ligation and puncture (CLP).
Cl-amidine also decreases the citrulline content in serum and joints and reduces the development of IgG autoantibodies in a mouse model of collagen-induced arthritis in a dose-dependent manner.

Physicochemical Properties

M.Wt 424.81
Formula C16H20ClF3N4O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2S)-5-(2-Chloroethanimidamido)-2-(phenylformamido)pentanamide trifluoroacetic acid salt

References

1. Yuan Luo, et al. Biochemistry. 2006 Oct 3; 45(39): 11727–11736.

2. Witalison EE, et al. Oncotarget. 2015 Nov 3;6(34):36053-62.

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