Cl-amidine

• Description:

  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].

• UNSPSC:

  12352005

• Hazard Statement:

  H302-H312-H315-H319-H332-H335

• Target:

  Apoptosis; MicroRNA; Protein Arginine Deiminase

• Type:

  Reference compound

• Related Pathways:

  Apoptosis; Epigenetics

• Applications:

  COVID-19-immunoregulation

• Field of Research:

  Cancer; Inflammation/Immunology

• Assay Protocol:

  https://www.medchemexpress.com/Cl-amidine.html

• Solubility:

  10 mM in DMSO

• Smiles:

  O=C(N[C@H](C(N)=O)CCCNC(CCl)=N)C1=CC=CC=C1

• Molecular Formula:

  C14H19ClN4O2

• Molecular Weight:

  310.78

• Precautions:

  P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362-P403+P233-P405-P501

• References & Citations:

  [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.

• Shipping Conditions:

  Room temperature

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Citation 01:

  Acta Pharm Sin B. 2025 Sep 12.|Eur Heart J. 2025 Oct 27:ehaf836.|Nat Biomed Eng. 2024 Sep;8 (9) :1177-1190.|Neoplasia. 2022 Nov;33:100835.|Research Square Print. January 4th, 2023.|Transl Res. 2023 May:255:85-96.|Vet Parasitol. 2022 Dec:312:109841.|Cell Rep. 2021 Sep 21;36 (12) :109750.|Chem Res Toxicol. 2022 Apr 18;35 (4) :597-605.|Exp Mol Med. 2024 Dec;56 (12) :2602-2616.|Fish Shellfish Immunol. 2022 Oct:129:22-29.|Free Radic Biol Med. 2024 Sep 12:S0891-5849 (24) 00656-7.|Immun Inflamm Dis. 2025 Nov;13 (11) :e70268.|Int Immunopharmacol. 2026 Jan 1;168 (Pt 1) :115862.|J Hazard Mater. 2025 Jan 16:487:137257.|MedComm (2020) . 2025 Jan 30;6 (2) :e70084.|Microb Pathogenesis. 2020 Dec;149:104530.|Microvasc Res. 2023 Nov:150:104592.

• CAS Number:

  [913723-61-2]