Cl-amidine,1373232-26-8

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Cl-amidine hydrochloride

CAS No. : 1373232-26-8

MCE 国际站：Cl-amidine hydrochloride

产品活性：Cl-amidine hydrochloride 是口服有效的 PAD 抑制剂，其对 PAD1、PAD3 和 PAD4 的 IC₅₀ 值分别为0.8 μM、 6.2 μM 和 5.9 μM。Cl-amidine hydrochloride 可诱导癌细胞的凋亡。Cl-amidine hydrochloride 可诱导 miR-16 (miRNA-16, microRNA-16)，引起细胞周期阻滞。Cl-Amidine hydrochloride 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。

研究领域：Epigenetics  |  Apoptosis

作用靶点：Protein Arginine Deiminase  |  Apoptosis  |  MicroRNA

In Vitro: Cl-amidine is a bioavailable haloacetamidine-based compound that inhibits all the active PAD isozymes with near equal potency (k_inact/K_I=13,000 M_-1 min-1 for PAD4).
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.
Cl-Amidine prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model.

In Vivo: Cl-amidine (75 mg/kg, ip once daily) suppresses and treats DSS-induced colitis in mice.
Cl-amidine (5, 25, 75 mg/kg, oral gavage, once daily) leads to significant reductions in the histology scores dose-dependently.

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