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 (53):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-157157
    PAD4-IN-3
    Inhibitor
    PAD4-IN-3 (compound 4B) is a PAD4 inhibitor with antitumor activity in vitro and in vivo. PAD4-IN-3 was covalently linked to RGD sequence peptide-modified chitosan (K-CRGDV), resulting in an enhanced oxidative stress-responsive nanoagent. K-CRGDV-PAD4-IN-3 can actively target tumors, inhibit PAD4 activity, block the formation of neutrophil extracellular traps (NETs), and improve the tumor immune microenvironment in response to the tumor microenvironment.
    PAD4-IN-3
  • HY-137125
    BB-Cl-Yne
    Inhibitor
    BB-Cl-Yne is a protein arginine deiminase (PAD) inhibitor with Ki values of PAD1-4.are 6400, 3600, 10800, 4900 M-1min-1 respectively. BB-Cl-Yne can be used as a click probe to label PAD.
    BB-Cl-Yne
  • HY-174349
    PAD-IN-3
    Inhibitor
    PAD-IN-3 (Compound 16) is a potent dual peptidyl arginine deiminases 4 (PAD4) and PAD1 inhibitor with IC50 values of 0.204 μM and 0.273 μM, respectively. PAD-IN-3 is promising for research of citrullination-associated disorders such as cancer and autoimmune diseases.
    PAD-IN-3
  • HY-171002A
    PAD2-IN-2 TFA
    Inhibitor
    PAD2-IN-2 (cis-isomer of 1) TFA is a protein arginine deiminase 2 (PAD2) inhibitor. PAD2-IN-2 TFA possess an azobenzene photoswitch to optically control PAD activity. PAD2-IN-2 TFA inhibits histone H3-citrullination.
    PAD2-IN-2 TFA
  • HY-B1505R
    Acefylline (Standard)
    Activator
    Acefylline (Standard) is the analytical standard of Acefylline. This product is intended for research and analytical applications. Acefylline, a xanthine derivative, is an adenosine receptor antagonist. Acefylline is a peptidylarginine deiminase (PAD) activator. Acefylline is also a bronchodilator and cardiac stimulant that inhibits rat lung cAMP phosphodiesterase isoenzymes. Acefylline can be used in asthma research.
    Acefylline (Standard)
  • 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-42034R
    Hydroquinine (Standard)
    Inhibitor
    Hydroquinine (Standard) is the analytical standard of Hydroquinine. Hydroquinine (Dihydroquinine) is an anti-bacterial agent that inhibits both Gram-positive and Gram-negative bacteria. Hydroquinine inhibits the growth of multidrug-resistant pseudomonas aeruginosa via the suppression of the arginine deiminase pathway genes. Hydroquinine inhibits Plasmodium falciparum and Plasmodium berghei. Hydroquinine displays anti-malarial and demelanizing activities. Hydroquinine effectively induces specific RND-type efflux pump systems in Pseudomonas aeruginosa, particularly the MexCD-OprJ and MexXY efflux pumps. Hydroquinine inhibits Pseudomonas aeruginosa adhesion and biofilm formation. Hydroquinine serves as a precursor for derivatives such as C9 epihydroquinine, 9-acetoxy-10,11-dihydroquinine, and 10,11-dihydroquinine monohydrochloride.
    Hydroquinine (Standard)
  • 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