1. Signaling Pathways
  2. Epigenetics
  3. Protein Arginine Deiminase

Protein Arginine Deiminase

Peptidylarginine Deiminase

Protein arginine deiminase (PAD), is a group of calcium-dependent enzymes, which play crucial roles in citrullination, and can catalyze arginine residues into citrulline. his chemical reaction induces citrullinated proteins formation with altered structure and function, leading to numerous pathological diseases, including inflammation and autoimmune diseases. These pathologies established the PADs as therapeutic targets and multiple PAD inhibitors are known.

Humans encode five PADs, designated PADs 1-4 and PAD6. Of the five PAD isozymes (PAD1, 2, 3, 4 and 6), only four (PADs1-4) are catalytically active. PAD activity is tightly regulated by Ca2+ and PADs contain 4 (PAD1), 5 (PAD3, 4) or 6 (PAD2) Ca2+-binding sites. Dysregulated PAD activity, most notably PAD2 and PAD4, is associated with multiple inflammatory diseases (e.g., rheumatoid arthritis) as well as cancer, and PAD inhibitors, such as Cl-amidine and BB-Cl-amidine, show efficacy in multiple preclinical animal models of disease.

Protein Arginine Deiminase Related Products (47):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-112903A
    YW3-56 hydrochloride
    Inhibitor
    YW3-56 (hydrochloride) is a PAD inhibitor. YW3-56 (hydrochloride) activates p53 target genes. YW3-56 (hydrochloride) activates ATF and blocks autophagy flux. YW3-56 induces ER stress through the PERK-eIF2α-ATF4 signaling cascade and inhibits the mTOR signaling. YW3-56 (hydrochloride) inhibits triple-negative breast cancer.
    YW3-56 hydrochloride
  • HY-137124
    BB-F-Yne
    Inhibitor
    BB-F-Yne is a protein arginine deiminase (PAD) inhibitor with Ki values of PAD1-4.are 2050, 1700, 1100, 3100 M-1min-1 respectively. BB-F-Yne can be used as a click probe to label PAD.
    BB-F-Yne
  • HY-169206
    PF-3166
    Inhibitor
    PF-3166 is a PAD2 inhibitor (IC50=150 nM) that is competitive with Ca2+. TPF-3166 insignificantly inhibits PAD3 or PAD4 (80 μM). PF-3166 also inhibits NH3 release (IC50=580 nM)..
    PF-3166
  • HY-171002
    PAD2-IN-2
    Inhibitor
    PAD2-IN-2 (cis-isomer of 1) is a protein arginine deiminase 2 (PAD2) inhibitor. PAD2-IN-2 possess an azobenzene photoswitch to optically control PAD activity. PAD2-IN-2 inhibits histone H3-citrullination.
    PAD2-IN-2
  • HY-126560
    F-Amidine
    Inhibitor
    F-Amidine is a Protein arginine deiminase 4 (PAD4) inhibitor. F-Amidine can be used in the study of inflammatory and immune system diseases (such as rheumatoid arthritis).
    F-Amidine
  • HY-B1505A
    Acefylline piperazine
    Activator
    Acefylline piperazine, a xanthine derivative, is an Adenosine Receptor antagonist. Acefylline piperazine is a peptidylarginine deiminase (PAD) activator. Acefylline piperazine is also a bronchodilator and cardiac stimulant that inhibits rat lung cAMP phosphodiesterase isoenzymes. Acefylline piperazine can be used in asthma research.
    Acefylline piperazine
  • HY-115676
    GSK199 analog hydrochloride
    Inhibitor
    GSK199 analog hydrochloride belongs to a class of compounds that inhibit PAD4 (guanidinoarginine deiminase 4). GSK199 analog hydrochloride has potential uses in diseases including rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosus, and psoriasis.
    GSK199 analog hydrochloride