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Pack Size | Price | Availability | Quantity |
---|---|---|---|
100 mg | Inquiry | 7-10 days | |
500 mg | Inquiry | 7-10 days |
Description | Cl-amidine TFA is an orally active inhibitor of peptidyl arginine deminase (PAD) 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. |
In vitro | Cl-amidine TFA inhibits all the active PAD isozymes with near equal potency (kinact/KI=13,000/(M?min) for PAD4) [1]. Cl-amidine (0, 5, 10, 15, 20, 25, 50 μg/mL, 24 hours) induces apoptosis in TK6 lymphoblastoid cells and HT29 colon cancer cells in a dose-dependent manner. Interestingly, the colon cancer cell line (HT29) is relatively resistant to apoptosis caused by Cl-amidine [2]. Cl-amidine irreversibly inactivates PADs by covalently modifying an active site cysteine that is important for its catalytic activity [4]. |
In vivo | Cl-amidine (75 mg/kg, i.p. once daily) suppresses and treats DSS-induced colitis in mice, and when administered via oral gavage at doses of 5, 25, and 75 mg/kg once daily, it dose-dependently reduces histology scores [2]. |
Molecular Weight | 424.8 |
Formula | C16H20ClF3N4O4 |
Cas No. | 1043444-18-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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