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CAS No.: 1373232-26-8

Cl-amidine HCl Catalog No. CSN37337

Synonyms: Cl-Amidine (hydrochloride);Cl-amidine HCl

Cl-amidine is an irreversible pan-peptidylarginine deiminase (PAD) inhibitor with IC50 values of with IC50 values of 5.9 ± 0.3 μM, 0.8 ± 0.3 μM, 6.2 ± 1.0 μM for PAD4, PAD1 and PAD3, respectively.

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实验方案

技术信息

生物活性

描述Cl-amidine is an irreversible pan-peptidylarginine deiminase (PAD) inhibitor with IC50 values of with IC50 values of 5.9 ± 0.3 μM, 0.8 ± 0.3 μM, 6.2 ± 1.0 μM for PAD4, PAD1 and PAD3, respectively^[1]. It is cytotoxic to HL-60, MCF-7, and HT-29 cancer cells (IC50s = 0.25, 0.05, and 1 μM, respectively)^[2]. Cl-amidine (0, 5, 10, 15, 20, 25, 50 μg/mL) induces apoptosis in TK6 lymphoblastoid cells and HT29 colon cancer cells in a dose-dependent manner. Cl-amidine (75 mg/kg) can significantly increase the levels of p21 and p53 in colonic epithelial inflammatory cells of colitis C57BL/6 mice, and induce apoptosis^[3].
动物研究
剂量
C57BL/6 mice 75 mg/kg (i.p.), 5, 25, 75mg/kg (p.o.) ^[3]

给药途径
i.p., p.o.
参考文献

动物研究
剂量	C57BL/6 mice 75 mg/kg (i.p.), 5, 25, 75mg/kg (p.o.) ^[3]
给药途径	i.p., p.o.

[1] Luo Y, Arita K, Bhatia M, Knuckley B, Lee YH, Stallcup MR, Sato M, Thompson PR. Inhibitors and inactivators of protein arginine deiminase 4: functional and structural characterization. Biochemistry. 2006 Oct 3;45(39):11727-36. doi: 10.1021/bi061180d. PMID: 17002273; PMCID: PMC1808342.
[2] Slack JL, Causey CP, Thompson PR. Protein arginine deiminase 4: a target for an epigenetic cancer therapy. Cell Mol Life Sci. 2011 Feb;68(4):709-20. doi: 10.1007/s00018-010-0480-x. Epub 2010 Aug 13. PMID: 20706768; PMCID: PMC3815436.
[3] Chumanevich AA, Causey CP, Knuckley BA, Jones JE, Poudyal D, Chumanevich AP, Davis T, Matesic LE, Thompson PR, Hofseth LJ. 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. doi: 10.1152/ajpgi.00435.2010. Epub 2011 Mar 17. PMID: 21415415; PMCID: PMC3119113.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8799 mL
- 14.3993 mL
- 28.7985 mL
- 5 mM
- 0.5760 mL
- 2.8799 mL
- 5.7597 mL
- 10 mM
- 0.2880 mL
- 1.4399 mL
- 2.8799 mL

技术信息

CAS号	1373232-26-8	储存条件	粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C14H20Cl2N4O2	运输	蓝冰
分子量	347.24	别名	Cl-Amidine (hydrochloride);Cl-amidine HCl

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