1. Epigenetics Apoptosis
  2. Protein Arginine Deiminase Apoptosis MicroRNA
  3. Cl-amidine

Cl-amidine 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 可诱导癌细胞的凋亡。Cl-amidine TFA 可诱导 miR-16 (miRNA-16, microRNA-16),引起细胞周期阻滞。Cl-Amidine 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。

该游离形式化合物不稳定,推荐具有相同生物学活性的稳定盐形式 Cl-amidine hydrochloride

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Cl-amidine Chemical Structure

Cl-amidine Chemical Structure

CAS No. : 913723-61-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Cl-amidine 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. Cl-amidine induces apoptosis in cancer cells. Cl-amidine induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model[1][2][3][4][5].

IC50 & Target

IC50: 0.8 μM (PAD1), 5.9 μM (PAD4), 6.2 μM (PAD3)[1][5].

体外研究
(In Vitro)

Cl-amidine is a bioavailable haloacetamidine-based compound that inhibits all the active PAD isozymes with near equal potency (kinact/KI=13,000 M-1•min-1 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[2].

Cell Line: TK6 lymphoblastoid cells and HT29 colon cancer cells.
Concentration: 0, 5, 10, 15, 20, 25, 50 μg/mL.
Incubation Time: 24 h.
Result: Induced apoptosis dose-dependently.
体内研究
(In Vivo)

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice (8-12 wk old, DSS mouse model of colitis)[2].
Dosage: 75 mg/kg.
Administration: IP once daily.
Result: Suppressed PAD activity, protein citrullination, and PAD levels in the colon in vivo.
Animal Model: C57BL/6 mice (8-12 wk old, DSS mouse model of colitis)[2].
Dosage: 5, 25, 75 mg/kg.
Administration: Oral gavage once daily.
Result: Led to significant reductions in the histology scores.
分子量

310.78

Formula

C14H19ClN4O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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