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Cl-amidine HCl

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Chemical Structure| 1373232-26-8 同义名 : Cl-Amidine (hydrochloride);Cl-amidine hydrochloride
CAS号 : 1373232-26-8
货号 : A835276
分子式 : C14H20Cl2N4O2
纯度 : 98%
分子量 : 347.24
MDL号 : MFCD22201084
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(143.99 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(143.99 mM)，配合低频超声助溶
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.88mL

0.58mL

0.29mL

14.40mL

2.88mL

1.44mL

28.80mL

5.76mL

2.88mL
参考文献

[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.