Cl-amidine (hydrochloride)

Cl-amidine hydrochloride 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 hydrochloride induces apoptosis in cancer cells. Cl-amidine hydrochloride induces microRNA (miR) -16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model[1][2][3][4][5].

Product Specifications

CAS Number

[1373232-26-8]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, 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_hydrochloride.html

Purity

99.82

Solubility

DMSO : 50 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

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

Molecular Formula

C14H20Cl2N4O2

Molecular Weight

347.25

Precautions

H302, H315, H319, H335

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.