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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。
Cl-amidine Chemical Structure
CAS No. : 913723-61-2
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
Cl-amidine 的其他形式现货产品:
Cl-amidine hydrochloride D-Cl-amidine hydrochloride
| 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].
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IC50 & Target |
IC50: 0.8 μM (PAD1), 5.9 μM (PAD4), 6.2 μM (PAD3)[1][5].
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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].
Shanghai Jinpan Biotech Co Ltd 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. |
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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].
Shanghai Jinpan Biotech Co Ltd 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. |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. Yuan Luo, et al. Inhibitors and Inactivators of Protein Arginine Deiminase 4: Functional and Structural Characterization. Biochemistry. 2006 Oct 3; 45(39): 11727–11736.
[2]. Chumanevich AA, et al. Suppression of colitis in mice by Cl-amidine: a novel peptidylarginine deiminase inhibitor. Am J Physiol Gastrointest Liver Physiol. 2011 Jun;300(6):G929-38.
[3]. Witalison EE, et al. Molecular targeting of protein arginine deiminases to suppress colitis and prevent colon cancer. Oncotarget. 2015 Nov 3;6(34):36053-62.
[4]. Biron BM, et al., Cl-Amidine Prevents Histone 3 Citrullination and Neutrophil Extracellular Trap Formation, and Improves Survival in a Murine Sepsis Model. J Innate Immun. 2017;9(1):22-32.
[5]. Bryan Knuckley, et al. Substrate Specificity and Kinetic Studies of PADs 1, 3, and 4 Identify Potent and Selective Inhibitors of Protein Arginine Deiminase 3. Biochemistry. 2010 Jun 15;49(23):4852-63.
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