Cl-amidine (TFA)

Cl-amidine (TFA)

• CAS Number: 1043444-18-3
• UNSPSC Description: Cl-amidine TFA 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 TFA induces apoptosis in cancer cells. Cl-amidine TFA induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine TFA prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model[1][2][3][4][5].
• Target Antigen: 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-tfa.html
• Solubility: 10 mM in DMSO
• Smiles: O=C(N[C@H](C(N)=O)CCCNC(CCl)=N)C1=CC=CC=C1.O=C(O)C(F)(F)F
• Molecular Weight: 424.80
• 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
• Clinical Information: No Development Reported