Cl-amidine hydrochloride 是一种口服有效的PAD抑制剂，可阻断组蛋白 3 瓜氨酸化和中性粒细胞胞外陷阱的形成，并提高败血症小鼠的存活率。它可诱导癌细胞凋亡，还可诱导 miR-16 引起细胞周期阻滞。

Cl-amidine hydrochloride is an orally active peptidylarginine deminase (PAD) inhibitor (IC50: 5.9 μM for PAD4). Cl-amidine hydrochloride induces apoptosis in cancer cells and it also induces microRNA (miR)-16 in vitro causing cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation. It improves survival in a murine sepsis model.

Cl-amidine, a bioavailable haloacetamidine-based compound, inhibits all the active PAD isozymes with near equal potency (kinact/KI=13,000 M-1?min-1 for PAD4)[1]. The colon cancer cell line (HT29) is relatively resistant to apoptosis caused by Cl-amidine[2]. 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.

Cl-amidine (5, 25, 75 mg/kg, oral gavage, once daily) causes significant reductions in the histology scores dose-dependently. Cl-amidine (75 mg/kg, ip once daily) inhibits and treats DSS-induced colitis in mice[2].

1373232-26-8

C14H20Cl2N4O2

347.24

H2O:50 mg/mL (143.99 mM),Need ultrasonic
DMSO:19.23 mg/mL (55.38 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years